Antengene Announces the Acceptance of ATG-010 (Selinexor) NDA by the NMPA for the Treatment of rrMM

On January 27, 2021 Antengene Corporation Limited ("Antengene", SEHK: 6996.HK), a leading innovative biopharmaceutical company dedicated to discovering, developing and commercializing global first-in-class and/or best-in class therapeutics in hematology and oncology, reported that the National Medical Products Administration (NMPA) accepted its New Drug Application (NDA) for ATG-010 (Selinexor, XPOVIO), a first-in-class oral selective inhibitor of nuclear export (SINE) compound, for the treatment of patients with relapsed/refractory multiple myeloma (rrMM) (Press release, Antengene, JAN 27, 2021, View Source [SID1234574357]). This is the fifth NDA for ATG-010 submitted by Antengene, after the four NDAs recently submitted in Australia, South Korea, Singapore and Hong Kong in the Asia Pacific region, and also the first NDA of SINE compounds in mainland China, a step closer to providing a novel option to Chinese patients diagnosed with hematological malignancies.

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Antengene has recently submitted NDAs in multiple markets for ATG-010 across three indications for multiple myeloma and diffuse large B-cell lymphoma. Recently, the National Comprehensive Cancer Network (NCCN) has also added five ATG-010 regimens to its guidelines for multiple myeloma or diffuse large B-cell lymphoma. ATG-010 is the first approved SINE compound in the world. It induces the apoptosis of cancer cells in vitro and in vivo by causing the nuclear storage and activation of tumor suppressor proteins and other growth-regulating proteins, and by down-regulating the intracytoplasmic levels of various oncogenic proteins while normal cells are not affected. Clinical studies have demonstrated that ATG-010 has clinical effects in multiple types of hematological and solid tumors with manageable safety profile.

"We are delighted to see the acceptance of the NDA submission in China for ATG-010 in rrMM, which marks another important milestone and one step closer to bringing ATG-010 to patients in China." said Dr. Jay Mei, M.D., Ph.D., Founder, Chairman and CEO of Antengene. "In addition to its effectiveness in hematological malignancies, there are several clinical trials in multiple solid tumor indications with ATG-010 including a global Phase 3 trial in endometrial cancer (SIENDO) and a Phase 3 trial in liposarcoma (SEAL) which have shown encouraging results. We continue to prepare to commercialize ATG-010 in China and across the APAC region so that cancer patients can benefit from this novel cancer medicine."

About ATG-010 (selinexor, XPOVIO)

ATG-010 (selinexor, XPOVIO), a first-in-class and only-in-class oral selective inhibitor of nuclear export (SINE) compound discovered and developed by Karyopharm Therapeutics Inc. (NASDAQ: KPTI), is currently being developed by Antengene, which has the exclusive development and commercial rights in certain Asia-Pacific markets, including Greater China, South Korea, Australia, New Zealand and the ASEAN countries.

In July 2019, the US Food and Drug Administration (FDA) approved selinexor (XPOVIO) in combination with low-dose dexamethasone for the treatment of relapsed/refractory multiple myeloma (rrMM) and in June 2020 approved selinexor (XPOVIO) as a single-agent for the treatment of relapsed/refractory diffuse large B-cell lymphoma (rrDLBCL). In December 2020, selinexor (XPOVIO) also received FDA approval as a combination treatment for multiple myeloma after at least one prior therapy. A Marketing Authorization Application (MAA) has also been submitted to the European Medicines Agency (EMA) with a request for conditional approval of selinexor in this same rrMM indication. Selinexor (XPOVIO) is so far the first and only oral SINE compound approved by the FDA and is the first drug approved for the treatment of both MM and DLBCL. Selinexor (XPOVIO) is also being evaluated in several other mid-and later-phase clinical trials across multiple solid tumor indications, including liposarcoma and endometrial cancer. In November 2020, at the Connective Tissue Oncology Society 2020 Annual Meeting (CTOS 2020), Antengene’s partner, Karyopharm, presented positive results from the Phase 3 randomized, double blind, placebo controlled, cross-over SEAL trial evaluating single agent, oral selinexor (XPOVIO) versus matching placebo in patients with liposarcoma. Karyopharm also announced that the ongoing Phase 3 SIENDO trial of selinexor (XPOVIO) in patients with endometrial cancer passed the planned interim futility analysis and the Data and Safety Monitoring Board (DSMB) recommended the trial should proceed as planned without any modifications. Top-line SIENDO trial results are expected in the second half of 2021.

Orexo Q4 2020, incl. Full Year Report

On January 27, 2021 Orexo reported that Q4 2020, incl. Full Year Report (Press release, Orexo, JAN 27, 2021, View Source [SID1234574355])

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Q4 2020 highlights

Total net revenues of SEK 159.2 m (238.1 last year, 196.2 m excl. Abstral EU and US)
Net earnings of SEK -49.6 m (38.9)
EBITDA of SEK 1.0 m (85.8)
US Pharma segment (ZUBSOLV US) net revenues of SEK 143.1 m (190.5), EBIT of SEK 94.4 m (95.5)
Cash flow from operating activities of SEK -11.2 m (60.2), cash balance of SEK 505.3 m (816.8)
Secured a preferred position for ZUBSOLV as the only branded product on national commercial and Medicare Part D formularies of the largest PBM in the commercial segment in the US, Express Script, from January 1, 2021
Finalized the technical development of modia, a digital therapy for opioid use disorder, for which Orexo owns the exclusive global rights
Entered an exclusive license and supply agreement with Accord Healthcare for ZUBSOLV covering 29 European countries
A new patent for ZUBSOLV, with protection until 2032, was issued by the US Patent and Trademark Office (USPTO)
Financial outlook provided for 2021, see page 14
Important events after the period

A new patent for OX124, overdose rescue medication, was issued by the USPTO protecting the technology until 2039
SEK m, unless otherwise stated

Progress while adjusting to new market dynamics

From a management perspective, the most important factor for success is to be an agile company, ready to accelerate development and to capture opportunities when they arise, but also be prepared to shift priorities when the market requires it. The quarter has seen progress on many fronts, with US Pharma showing net revenue growth in local currency comparing to last quarter and improved EBIT margin, Digital Therapeutics (DTx) testing new reimbursement routes and launching new commercialization concepts. Our lead pipeline project, a rescue medication for opioid overdose, OX124, received positive feedback from the FDA on the IND application enabling a request for Fast Track Designation of the product and we also reported an exclusive license and supply agreement for ZUBSOLV in Europe.

Strong financial base to enable investments in DTx and launch of OX124

Our full year OPEX was SEK 617 million, which is significantly less than the guidance of SEK 750-800 million communicated in our Q2 report. The guidance in Q2 was based on the significant interest in DTx in the beginning of the Covid-19 pandemic and our expectation that payers and healthcare providers would follow the FDA’s decision to include digital therapies under the Public Health Emergency Policy and find pragmatic routes for reimbursement. While the interest in Orexo’s digital therapies remains high, building a new market requires patience. We start to see concrete and promising development with regards to DTx reimbursement, which is a cornerstone to accelerate growth.

Looking ahead, we expect to increase the investment in DTx as we see a progression in sales and a clearer picture emerges regarding the multiple routes to reimbursement. 2021 will also require significant investments in OX124, as we enter the pivotal trial starting in the summer this year. To ensure we have financial headroom to invest in opportunities when they arise, both internally in our products and our pipeline and through business development, we intend to refinance our existing corporate bond during Q1 2021 with a new corporate bond issue.

Expanding the commercialization model in DTx

The expectations of our DTx portfolio in 2020 were boosted by the FDA’s decision to implement a Public Health Emergency Policy allowing commercialization of digital therapies within the CNS space without the ordinary approval process. We anticipated that the payers would adopt similar pragmatism to the reimbursement processes as a response to the Public Health Emergency Policy, but the reimbursement process is following the pattern we anticipated before Covid-19, i.e. a new disruptive treatment will take time to review and implement. As a result, we are testing several new concepts for reimbursement of our digital therapies in parallel, while making the DTx available through direct purchase for patients. The lead concept is a treatment program where we, in collaboration with selected healthcare providers, offer patients treatment under the supervision of a physician. Provided the physicians and the patients follow certain guidelines, this treatment program is currently available for reimbursement for a large portion of the US population. The program is being tested in Pennsylvania to a limited number of patients to ensure the reimbursement will follow the expected path before we launch nationwide. The same program will also be available for individual physicians to treat patients under a direct contract with Orexo. In addition to this program, we are finalizing a program for employers, working with patient to patient communication, and continue our work with payers to drive reimbursement.

ZUBSOLV decline diminishing while impact of Covid-19 continues

With bipartisan support for the ongoing opioid crisis in the US, I am pleased to see politicians returning their attention to the opioid crisis. The former US administration recently paved the way for all US physicians to prescribe medical-assisted treatment (MAT) for opioid dependence, and we are confident that in the event of changes under the new administration, addressing the opioid crisis will remain a key priority. With the ongoing Covid-19 pandemic having significantly worsened this crisis, there is a pressing need increase access to treatment. Such a change will likely drive a sustained strong market growth, which will benefit Orexo and ZUBSOLV.

This quarter we had a small net sales increase compared to Q3 and a strong EBIT margin of 66 percent. Apart from some one-time adjustments, this result is explained by minimal decline from former exclusive contracts and stable development in the open segment. When Covid-19 is behind us, we expect a stabilization of the business and growth. ZUBSOLV is the only promoted daily treatment in opioid dependence in the US, and Covid-19 restrictions have had a severe impact on our ability to promote the product. In combination with our core market segment, the commercial segment, being stagnant due to the unemployment caused by Covid-19, it is a challenging market place during the pandemic. However, the Covid-19 challenges also provides learning of how to be more efficient in the sales process, which will benefit us long term. We expect ZUBSOLV will continue to be an important EBIT contributor in the years to come and with the broad launch of modia, our digital therapy for opioid use disorder, in the second half of 2021 we will see increased commercial synergies between our digital therapies and ZUBSOLV, both from a cost and revenue perspective.

OX124 development progressing to plan

As the US death tolls associated with overdose of fentanyl continue, we are confident OX124 is urgently needed, with the promise of being the most powerful nasal delivery of naloxone in the market. I am very pleased with the progress we have made during the quarter. With continued progress according to plan, in Q1 2021 we will receive a decision on the Fast Track application, continue to establish a commercial supply chain, improve the IP protection and register the brand name for OX124. In Q2 2021 we will manufacture the batches required for regulatory stability data and we will start the pivotal clinical trial. If the Fast Track application is approved we will be ready to submit an application for approval in Q1 2022. Without Fast Track the process will be delayed as we expect the FDA will require additional stability data to support proposed shelf life of the commercial product.

Summary and Outlook

In the last quarterly report I highlighted the pressing need for Orexo’s products as a result of the Covid-19 pandemic. The Covid-19 pandemic has unfortunately escalated, and the need for our products is even greater than before. The delays to get the DTx products reimbursement is certainly frustrating, especially given the clear demand for such products in the current climate. However, I also have to respect that Covid-19 has had a severe impact on many organizations and their ability to operate as normal. This aside, we are encouraged by the positive feedback we receive from customers and the steady progression we see in the number of patients testing and buying our DTx products in January. I remain confident that 2021 will show the commercial potential of these products, while we continue to enjoy strong and stable EBIT contribution from ZUBSOLV and prepare the new drug application for OX124.Uppsala, Sweden,

Presentation

At 2.00 pm CET, the same day as the announcement of the report, Orexo invites analysts, investors and media to attend an audiocast with a web presentation where Nikolaj Sørensen, CEO, and Joseph DeFeo, CFO, will present the report. After the presentation a Q&A will be held. Questions can also be sent in advance to [email protected], no later than 11.00 am CET. Please view the instructions below on how to participate.Internet: View Source SE +46 8 50 558 358 UK +44 333 300 9267 US +1 833 249 8403 The presentation material will be available on Orexo’s website prior to the audiocast, view Investors/Reports, presentations and audicastsThis information is information that Orexo AB (publ.) is obliged to make public pursuant to the EU Market Abuse Regulation. The information was submitted for publication, through the agency of the contact persons set out above, at 8.00 am CET on January 28, 2021.

BeiGene Announces Positive Topline Results for Global Phase 3 Trial of Tislelizumab in Esophageal Squamous Cell Carcinoma

On January 27, 2021 BeiGene, Ltd. (NASDAQ: BGNE; HKEX: 06160), a commercial-stage biotechnology company focused on developing and commercializing innovative medicines worldwide, reported that the global Phase 3 RATIONALE 302 trial of its anti-PD-1 antibody tislelizumab versus investigator’s choice chemotherapy in patients with advanced unresectable or metastatic esophageal squamous cell carcinoma (ESCC) who have received prior systemic treatment met its primary endpoint of overall survival (OS) (Press release, BeiGene, JAN 27, 2021, View Source [SID1234574354]). In the trial results, tislelizumab demonstrated a statistically significant and clinically meaningful improvement in OS in the intention-to-treat (ITT) population, when compared to chemotherapy. The safety profile of tislelizumab was consistent with its known risks, with no new safety signals identified.

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"With our ongoing evaluation of tislelizumab across multiple tumor types, we are working to provide clinical evidence and bring this potentially differentiated anti-PD-1 antibody to far more patients around the world."

"We are excited to announce the improved overall survival observed in another Phase 3 trial for tislelizumab when compared to chemotherapy standard of care. This is our fourth positive Phase 3 readout for tislelizumab and the first from our large Phase 3 program in gastrointestinal cancers that also include liver, stomach cancers as well as esophageal cancer," commented Yong (Ben) Ben, M.D., Chief Medical Officer, Immuno-Oncology at BeiGene. "With our ongoing evaluation of tislelizumab across multiple tumor types, we are working to provide clinical evidence and bring this potentially differentiated anti-PD-1 antibody to far more patients around the world."

BeiGene plans to discuss the RATIONALE 302 data with health authorities globally and present data at an upcoming medical conference.

"Esophageal cancer represents a significant unmet medical need with rapid progression and high mortality. Recent years have seen a paradigm-shift in advanced ESCC treatment from chemotherapy and radiation to immunotherapy. The positive topline results from the RATIONALE 302 trial demonstrated that tislelizumab may offer a new treatment option for those living with this devastating disease and bring hope to patients and their families," said Lin Shen, M.D., Vice President of Clinical Oncology at Beijing Cancer Hospital and lead investigator for the trial.

RATIONALE 302 Trial of Tislelizumab Versus Chemotherapy in Advanced ESCC

RATIONALE 302 is a randomized, open-label, multicenter global Phase 3 trial (NCT03430843) designed to evaluate the efficacy and safety of tislelizumab when compared to investigator’s choice chemotherapy in patients with advanced unresectable or metastatic ESCC who have received prior systemic treatment.

The primary endpoint of the trial is OS in the ITT population. A total of 512 patients enrolled in the trial in 11 countries across Asia, Europe, and North America, randomized 1:1 to either the tislelizumab arm or the chemotherapy arm (investigator’s choice of paclitaxel, docetaxel, or irinotecan).

About Esophageal Squamous Cell Carcinoma (ESCC)

Esophageal squamous cell carcinoma (ESCC) is the most common subtype of esophageal cancer globally, the sixth leading cause of cancer-related death in the world.i In 2020, there were more than 600,000 new cases of esophageal cancer and approximately 550,000 deaths worldwide.ii Esophageal cancer is a rapidly fatal disease and more than two-thirds of the patients have advanced or metastatic disease at the time of diagnosis, with a median survival of eight to 10 months and an expected five-year survival rate of less than five percent.iii

About Tislelizumab

Tislelizumab (BGB-A317) is a humanized IgG4 anti-PD-1 monoclonal antibody specifically designed to minimize binding to FcγR on macrophages. In pre-clinical studies, binding to FcγR on macrophages has been shown to compromise the anti-tumor activity of PD-1 antibodies through activation of antibody-dependent macrophage-mediated killing of T effector cells. Tislelizumab is the first drug from BeiGene’s immuno-oncology biologics program and is being developed internationally as a monotherapy and in combination with other therapies for the treatment of a broad array of both solid tumor and hematologic cancers.

The China National Medical Products Administration (NMPA) has granted tislelizumab full approval for first-line treatment of patients with advanced squamous non-small cell lung cancer (NSCLC) in combination with chemotherapy. Tislelizumab has also received conditional approval from the NMPA for the treatment of patients with classical Hodgkin’s lymphoma who received at least two prior therapies and for the treatment of patients with locally advanced or metastatic urothelial carcinoma with PD-L1 high expression whose disease progressed during or following platinum-containing chemotherapy or within 12 months of neoadjuvant or adjuvant treatment with platinum-containing chemotherapy. Full approval for these indications is contingent upon results from ongoing randomized, controlled confirmatory clinical trials.

In addition, two supplemental new drug applications for tislelizumab have been accepted by the Center for Drug Evaluation (CDE) of the NMPA and are under review for first-line treatment of patients with advanced non-squamous NSCLC in combination with chemotherapy, and for previously treated unresectable hepatocellular carcinoma.

Currently, 15 potentially registration-enabling clinical trials are being conducted in China and globally, including 13 Phase 3 trials and two pivotal Phase 2 trials.

In January 2021, BeiGene and Novartis entered into a collaboration and license agreement to develop, manufacture, and commercialize tislelizumab in North America, Europe, and Japan, and the transaction is expected to close in the first quarter of 2021, subject to expiration or early termination of the waiting period under the Hart-Scott-Rodino Antitrust Improvements Act.

Tislelizumab is not approved for use outside of China.

About Tislelizumab Clinical Program

Clinical trials of tislelizumab include:

Phase 3 trial comparing tislelizumab to salvage chemotherapy in patients with relapsed/refractory classical Hodgkin Lymphoma (NCT04486391);
Phase 3 trial in patients with locally advanced or metastatic urothelial carcinoma (NCT03967977);
Phase 3 trial comparing tislelizumab with docetaxel in the second- or third-line setting in patients with NSCLC (NCT03358875);
Phase 3 trial of tislelizumab in combination with chemotherapy versus chemotherapy as first-line treatment for patients with advanced squamous NSCLC (NCT03594747);
Phase 3 trial of tislelizumab in combination with chemotherapy versus chemotherapy as first-line treatment for patients with advanced non-squamous NSCLC (NCT03663205);
Phase 3 trial of tislelizumab in combination with platinum-based doublet chemotherapy as neoadjuvant treatment for patients with NSCLC (NCT04379635);
Phase 3 trial of tislelizumab combined with platinum and etoposide versus placebo combined with platinum and etoposide in patients with extensive-stage small cell lung cancer (NCT04005716);
Phase 3 trial comparing tislelizumab with sorafenib as first-line treatment for patients with hepatocellular carcinoma (HCC; NCT03412773);
Phase 2 trial in patients with previously treated unresectable HCC (NCT03419897);
Phase 3 trial comparing tislelizumab with chemotherapy as second-line treatment for patients with advanced esophageal squamous cell carcinoma (ESCC; NCT03430843);
Phase 3 trial of tislelizumab in combination with chemotherapy as first-line treatment for patients with ESCC (NCT03783442);
Phase 3 trial of tislelizumab versus placebo in combination with chemoradiotherapy in patients with localized ESCC (NCT03957590);
Phase 3 trial of tislelizumab combined with chemotherapy versus placebo combined with chemotherapy as first-line treatment for patients with gastric cancer (NCT03777657);
Phase 2 trial in patients with MSI-H/dMMR solid tumors (NCT03736889); and
Phase 3 trial of tislelizumab combined with chemotherapy versus placebo combined with chemotherapy as first-line treatment in patients with nasopharyngeal cancer (NCT03924986).

Head-to-Head Study Shows Guardant360 Liquid Biopsy Outperforms Tissue Biopsy for Comprehensive Genomic Profiling in Advanced Non-Small Cell Lung Cancer with Similar Outcomes

On January 27, 2021 Guardant Health, Inc. (Nasdaq: GH) reported that Despite guideline recommendations for comprehensive genomic profiling (CGP) of all patients with advanced non-small cell lung cancer (NSCLC), profiling remains suboptimal due to continued reliance on invasive tissue biopsies for testing (Press release, Guardant Health, JAN 27, 2021, View Source [SID1234574353]). A new study published in JCO Precision Oncology confirms previously reported data showing that the Guardant360 liquid biopsy is not only concordant to tissue genotyping, but detects significantly more informative alterations when used prior to tissue testing, and achieves similar treatment response rates and progression-free survival in patients with NSCLC. Publication link here.

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The prospective study1 (n=186) compares comprehensive genomic profiling using the Guardant360 liquid biopsy versus standard-of-care tissue genotyping for first-line treatment decisions in advanced NSCLC. Patients with advanced NSCLC received targeted therapies based on the actionable biomarkers identified. Compared to tissue biopsy genotyping at time of diagnoses, the Guardant360 liquid biopsy was not only concordant with tissue biopsy but detected 23.6 percent more informative mutations when used first and before tissue biopsy.

The study adds to the growing body of evidence2-4 demonstrating that using a "blood-first approach" using the Guardant360 test for genomic biomarker detection can identify more actionable biomarkers than a "tissue-first approach". Importantly, objective response rates and progression-free survival in biomarker-positive patients receiving targeted therapy was similar to previously reported registrational trials.

"Despite the ever-growing availability of life-changing targeted drugs for treating patients with advanced lung cancer, many continue to be treated with chemotherapy or immunotherapy because first-line treatments are made without conducting comprehensive genotyping first," said the Principal Investigator of this study Dr. Rafael Rossell, Chief Medical Officer and President of the Dr. Rosell Oncology Institute. "This publication outlines further evidence that the Guardant Health liquid biopsy is very effective in uncovering actionable genomic alterations, overcomes the challenges of tissue biopsies, and helps clinicians more easily customize treatments to improve the prognosis and survival of their patients."

Numerous clinical studies show that patients receiving targeted or personalized treatments have improved progression-free survival and higher overall response rates compared to chemotherapy or immunotherapy.5-11 Various factors contribute to clinical adoption of personalized medicine lagging behind recommended medical guidelines, including insufficient tissue for biopsy, which is the case for as many as 30 percent of solid cancer patients.12-14

"Once again, the data show that our blood-first approach using our Guardant360 liquid biopsy has the advantage of increasing the number of patients receiving potentially life-changing targeted treatments without compromising treatment efficacy," said Helmy Eltoukhy, Guardant Health CEO. "Sadly, research indicates that approximately 80 percent of advanced lung cancer patients do not receive comprehensive genotyping before starting treatment. I hope that with the recent FDA approval of our Guardant360 CDx liquid biopsy test, more clinicians will feel confident making the shift to liquid biopsies so we can reverse the serious trend of undergenotyping that exists today."

ENHERTU® Receives Prime Minister’s Award from the Japan Techno-Economics Society

On January 27, 2021 Daiichi Sankyo Company, Limited (hereafter, Daiichi Sankyo) reported that ENHERTU (trastuzumab deruxtecan), a HER2 directed antibody drug conjugate (ADC), received the Prime Minister’s Award at the 9th Technology Management and Innovation Awards hosted by the Japan Techno-Economics Society (JATES) (Press release, Daiichi Sankyo, JAN 27, 2021, View Source [SID1234574349]).

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The Technology Management and Innovation Awards were established in 2012 with the objective of contributing to the development of the nation’s economy, social changes, and the promotion of a global competitive edge by widely introducing technological innovations originating in Japan. This year marks the 9th year of the award.

"It is a great honor for us to receive such a prestigious award," said Sunao Manabe, Representative Director, President and CEO of Daiichi Sankyo Company, Limited. "We have been evaluated for our wide array of efforts and initiatives to offer promising treatment options to patients with cancer for whom the range of therapies is limited. We will continue to work hard to deliver therapies for more indications to patients around the world."

Daiichi Sankyo received this award as a result of several key accomplishments achieved through the comprehensive research and development program for ENHERTU. These accomplishments included the development of a management system that enabled rapid decision-making for the technological research and development of ENHERTU; collaborating with academic and healthcare institutions to create quality non-clinical and clinical data that met international standards to secure regulatory approvals; exploring new and innovative ways to deliver ENHERTU to patients as quickly as possible; and developing a successful formula to minimize quality risk.

About ENHERTU
ENHERTU (5.4 mg/kg; T-DXd; trastuzumab deruxtecan; fam-trastuzumab deruxtecan-nxki in the U.S. only) is approved in the U.S. under accelerated approval, in the EU under conditional marketing authorization, and in Japan under the conditional early approval system for the treatment of adult patients with unresectable or metastatic HER2 positive breast cancer who have received two or more prior anti-HER2 based regimens in the metastatic setting based on the results from the DESTINY-Breast01 trial.

ENHERTU (6.4 mg/kg) is also approved in the U.S. and Japan for the treatment of patients with HER2 positive unresectable advanced or recurrent gastric cancer who have received a prior trastuzumab-based regimen based on the results from the DESTINY-Gastric01 trial.

ENHERTU is approved in the U.S. with Boxed WARNINGS for Interstitial Lung Disease and Embryo-Fetal Toxicity.

About the ENHERTU Clinical Development Program
A comprehensive development program is underway globally with nine pivotal trials evaluating the efficacy and safety of ENHERTU monotherapy across multiple HER2 targetable cancers including breast, gastric and lung cancers. Trials in combination with other anticancer treatments, such as immunotherapy, are also underway.

In May 2020, ENHERTU received Breakthrough Therapy Designation (BTD) in the U.S. for the treatment of patients with metastatic non-small cell lung cancer whose tumors have a HER2 mutation and with disease progression on or after platinum-based therapy.

About the Daiichi Sankyo and AstraZeneca Collaboration
ENHERTU (T-DXd; trastuzumab deruxtecan; fam-trastuzumab deruxtecan-nxki in the U.S. only) and datopotamab deruxtecan (Dato-DXd; DS-1062) are two lead DXd ADCs in the oncology pipeline of Daiichi Sankyo, and the most advanced programs in AstraZeneca’s ADC scientific platform.

Each ADC is engineered using Daiichi Sankyo’s proprietary and portable DXd ADC technology to target and deliver chemotherapy inside cancer cells that express a specific cell surface antigen. Both ENHERTU (a HER2 directed ADC) and datopotamab deruxtecan (a TROP2 directed ADC) consist of a monoclonal antibody attached to a topoisomerase I inhibitor payload, an exatecan derivative, via a stable tetrapeptide-based cleavable linker.

Daiichi Sankyo and AstraZeneca entered into a global collaboration to jointly develop and commercialize ENHERTU in March 2019, and datopotamab deruxtecan in July 2020, except in Japan where Daiichi Sankyo maintains exclusive rights for each ADC. Daiichi Sankyo is responsible for manufacturing and supply of ENHERTU and datopotamab deruxtecan.

Datopotamab deruxtecan is an investigational agent that has not been approved for any indication in any country. Safety and efficacy have not been established.

U.S. Important Safety Information for ENHERTU

Indications
ENHERTU is a HER2-directed antibody and topoisomerase inhibitor conjugate indicated for the treatment of adult patients with:

Unresectable or metastatic HER2-positive breast cancer who have received two or more prior anti-HER2-based regimens in the metastatic setting.

This indication is approved under accelerated approval based on tumor response rate and duration of response. Continued approval for this indication may be contingent upon verification and description of clinical benefit in a confirmatory trial.
Locally advanced or metastatic HER2-positive gastric or gastroesophageal junction adenocarcinoma who have received a prior trastuzumab-based regimen.
WARNING: INTERSTITIAL LUNG DISEASE and EMBRYO-FETAL TOXICITY

Interstitial lung disease (ILD) and pneumonitis, including fatal cases, have been reported with ENHERTU. Monitor for and promptly investigate signs and symptoms including cough, dyspnea, fever, and other new or worsening respiratory symptoms. Permanently discontinue ENHERTU in all patients with Grade 2 or higher ILD/pneumonitis. Advise patients of the risk and to immediately report symptoms.
Exposure to ENHERTU during pregnancy can cause embryo-fetal harm. Advise patients of these risks and the need for effective contraception.
Contraindications
None.

Warnings and Precautions
Interstitial Lung Disease / Pneumonitis
Severe, life-threatening, or fatal interstitial lung disease (ILD), including pneumonitis, can occur in patients treated with ENHERTU. Advise patients to immediately report cough, dyspnea, fever, and/or any new or worsening respiratory symptoms. Monitor patients for signs and symptoms of ILD. Promptly investigate evidence of ILD. Evaluate patients with suspected ILD by radiographic imaging. Consider consultation with a pulmonologist. For asymptomatic ILD/pneumonitis (Grade 1), interrupt ENHERTU until resolved to Grade 0, then if resolved in ≤28 days from date of onset, maintain dose. If resolved in >28 days from date of onset, reduce dose one level. Consider corticosteroid treatment as soon as ILD/pneumonitis is suspected (e.g., ≥0.5 mg/kg/day prednisolone or equivalent). For symptomatic ILD/pneumonitis (Grade 2 or greater), permanently discontinue ENHERTU. Promptly initiate systemic corticosteroid treatment as soon as ILD/pneumonitis is suspected (e.g., ≥1 mg/kg/day prednisolone or equivalent) and continue for at least 14 days followed by gradual taper for at least 4 weeks.

Metastatic Breast Cancer
In clinical studies, of the 234 patients with unresectable or metastatic HER2-positive breast cancer treated with ENHERTU 5.4 mg/kg, ILD occurred in 9% of patients. Fatal outcomes due to ILD and/or pneumonitis occurred in 2.6% of patients treated with ENHERTU. Median time to first onset was 4.1 months (range: 1.2 to 8.3).

Locally Advanced or Metastatic Gastric Cancer
In DESTINY-Gastric01, of the 125 patients with locally advanced or metastatic HER2‑positive gastric or GEJ adenocarcinoma treated with ENHERTU 6.4 mg/kg, ILD occurred in 10% of patients. Median time to first onset was 2.8 months (range: 1.2 to 21.0).

Neutropenia
Severe neutropenia, including febrile neutropenia, can occur in patients treated with ENHERTU. Monitor complete blood counts prior to initiation of ENHERTU and prior to each dose, and as clinically indicated. For Grade 3 neutropenia (Absolute Neutrophil Count [ANC] <1.0 to 0.5 x 109/L) interrupt ENHERTU until resolved to Grade 2 or less, then maintain dose. For Grade 4 neutropenia (ANC <0.5 x 109/L) interrupt ENHERTU until resolved to Grade 2 or less. Reduce dose by one level. For febrile neutropenia (ANC <1.0 x 109/L and temperature >38.3ºC or a sustained temperature of ≥38ºC for more than 1 hour), interrupt ENHERTU until resolved. Reduce dose by one level.

Metastatic Breast Cancer
In clinical studies, of the 234 patients with unresectable or metastatic HER2-positive breast cancer who received ENHERTU 5.4mg/kg, a decrease in neutrophil count was reported in 62% of patients. Sixteen percent had Grade 3 or 4 decrease in neutrophil count. Median time to first onset of decreased neutrophil count was 23 days (range: 6 to 547). Febrile neutropenia was reported in 1.7% of patients.

Locally Advanced or Metastatic Gastric Cancer
In DESTINY-Gastric01, of the 125 patients with locally advanced or metastatic HER2‑positive gastric or GEJ adenocarcinoma treated with ENHERTU 6.4 mg/kg, a decrease in neutrophil count was reported in 72% of patients. Fifty-one percent had Grade 3 or 4 decreased neutrophil count. Median time to first onset of decreased neutrophil count was 16 days (range: 4 to 187). Febrile neutropenia was reported in 4.8% of patients.

Left Ventricular Dysfunction
Patients treated with ENHERTU may be at increased risk of developing left ventricular dysfunction. Left ventricular ejection fraction (LVEF) decrease has been observed with anti-HER2 therapies, including ENHERTU. In the 234 patients with unresectable or metastatic HER2-positive breast cancer who received ENHERTU, two cases (0.9%) of asymptomatic LVEF decrease were reported. In DESTINY-Gastric01, of the 125 patients with locally advanced or metastatic HER2‑positive gastric or GEJ adenocarcinoma treated with ENHERTU 6.4 mg/kg, no clinical adverse events of heart failure were reported; however, on echocardiography, 8% were found to have asymptomatic Grade 2 decrease in LVEF. Treatment with ENHERTU has not been studied in patients with a history of clinically significant cardiac disease or LVEF <50% prior to initiation of treatment.

Assess LVEF prior to initiation of ENHERTU and at regular intervals during treatment as clinically indicated. When LVEF is >45% and absolute decrease from baseline is 10-20%, continue treatment with ENHERTU. When LVEF is 40-45% and absolute decrease from baseline is <10%, continue treatment with ENHERTU and repeat LVEF assessment within 3 weeks. When LVEF is 40-45% and absolute decrease from baseline is 10-20%, interrupt ENHERTU and repeat LVEF assessment within 3 weeks. If LVEF has not recovered to within 10% from baseline, permanently discontinue ENHERTU. If LVEF recovers to within 10% from baseline, resume treatment with ENHERTU at the same dose. When LVEF is <40% or absolute decrease from baseline is >20%, interrupt ENHERTU and repeat LVEF assessment within 3 weeks. If LVEF of <40% or absolute decrease from baseline of >20% is confirmed, permanently discontinue ENHERTU. Permanently discontinue ENHERTU in patients with symptomatic congestive heart failure.

Embryo-Fetal Toxicity
ENHERTU can cause fetal harm when administered to a pregnant woman. Advise patients of the potential risks to a fetus. Verify the pregnancy status of females of reproductive potential prior to the initiation of ENHERTU. Advise females of reproductive potential to use effective contraception during treatment and for at least 7 months following the last dose of ENHERTU. Advise male patients with female partners of reproductive potential to use effective contraception during treatment with ENHERTU and for at least 4 months after the last dose of ENHERTU.

Additional Dose Modifications
Thrombocytopenia
For Grade 3 thrombocytopenia (platelets <50 to 25 x 109/L) interrupt ENHERTU until resolved to Grade 1 or less, then maintain dose. For Grade 4 thrombocytopenia (platelets <25 x 109/L) interrupt ENHERTU until resolved to Grade 1 or less. Reduce dose by one level.

Adverse Reactions
Metastatic Breast Cancer
The safety of ENHERTU was evaluated in a pooled analysis of 234 patients with unresectable or metastatic HER2-positive breast cancer who received at least one dose of ENHERTU 5.4 mg/kg in DESTINY-Breast01 and Study DS8201-A-J101. ENHERTU was administered by intravenous infusion once every three weeks. The median duration of treatment was 7 months (range: 0.7 to 31).

Serious adverse reactions occurred in 20% of patients receiving ENHERTU. Serious adverse reactions in >1% of patients who received ENHERTU were interstitial lung disease, pneumonia, vomiting, nausea, cellulitis, hypokalemia, and intestinal obstruction. Fatalities due to adverse reactions occurred in 4.3% of patients including interstitial lung disease (2.6%), and the following events occurred in one patient each (0.4%): acute hepatic failure/acute kidney injury, general physical health deterioration, pneumonia, and hemorrhagic shock.

ENHERTU was permanently discontinued in 9% of patients, of which ILD accounted for 6%. Dose interruptions due to adverse reactions occurred in 33% of patients treated with ENHERTU. The most frequent adverse reactions (>2%) associated with dose interruption were neutropenia, anemia, thrombocytopenia, leukopenia, upper respiratory tract infection, fatigue, nausea, and ILD. Dose reductions occurred in 18% of patients treated with ENHERTU. The most frequent adverse reactions (>2%) associated with dose reduction were fatigue, nausea, and neutropenia.

The most common (≥20%) adverse reactions, including laboratory abnormalities, were nausea (79%), white blood cell count decreased (70%), hemoglobin decreased (70%), neutrophil count decreased (62%), fatigue (59%), vomiting (47%), alopecia (46%), aspartate aminotransferase increased (41%), alanine aminotransferase increased (38%), platelet count decreased (37%), constipation (35%), decreased appetite (32%), anemia (31%), diarrhea (29%), hypokalemia (26%), and cough (20%).

Locally Advanced or Metastatic Gastric Cancer
The safety of ENHERTU was evaluated in 187 patients with locally advanced or metastatic HER2‑positive gastric or GEJ adenocarcinoma in DESTINY‑Gastric01. Patients intravenously received at least one dose of either ENHERTU (N=125) 6.4 mg/kg once every three weeks or either irinotecan (N=55) 150 mg/m2 biweekly or paclitaxel (N=7) 80 mg/m2 weekly for 3 weeks. The median duration of treatment was 4.6 months (range: 0.7 to 22.3) in the ENHERTU group and 2.8 months (range: 0.5 to 13.1) in the irinotecan/paclitaxel group.

Serious adverse reactions occurred in 44% of patients receiving ENHERTU 6.4 mg/kg. Serious adverse reactions in >2% of patients who received ENHERTU were decreased appetite, ILD, anemia, dehydration, pneumonia, cholestatic jaundice, pyrexia, and tumor hemorrhage. Fatalities due to adverse reactions occurred in 2.4% of patients: disseminated intravascular coagulation, large intestine perforation, and pneumonia occurred in one patient each (0.8%).

ENHERTU was permanently discontinued in 15% of patients, of which ILD accounted for 6%. Dose interruptions due to adverse reactions occurred in 62% of patients treated with ENHERTU. The most frequent adverse reactions (>2%) associated with dose interruption were neutropenia, anemia, decreased appetite, leukopenia, fatigue, thrombocytopenia, ILD, pneumonia, lymphopenia, upper respiratory tract infection, diarrhea, and hypokalemia. Dose reductions occurred in 32% of patients treated with ENHERTU. The most frequent adverse reactions (>2%) associated with dose reduction were neutropenia, decreased appetite, fatigue, nausea, and febrile neutropenia.

The most common (≥20%) adverse reactions, including laboratory abnormalities, were hemoglobin decreased (75%), white blood cell count decreased (74%), neutrophil count decreased (72%), lymphocyte count decreased (70%), platelet count decreased (68%), nausea (63%), decreased appetite (60%), anemia (58%), aspartate aminotransferase increased (58%), fatigue (55%), blood alkaline phosphatase increased (54%), alanine aminotransferase increased (47%), diarrhea (32%), hypokalemia (30%), vomiting (26%), constipation (24%), blood bilirubin increased (24%), pyrexia (24%), and alopecia (22%).

Use in Specific Populations

Pregnancy: ENHERTU can cause fetal harm when administered to a pregnant woman. Advise patients of the potential risks to a fetus. There are clinical considerations if ENHERTU is used in pregnant women, or if a patient becomes pregnant within 7 months following the last dose of ENHERTU.
Lactation: There are no data regarding the presence of ENHERTU in human milk, the effects on the breastfed child, or the effects on milk production. Because of the potential for serious adverse reactions in a breastfed child, advise women not to breastfeed during treatment with ENHERTU and for 7 months after the last dose.
Females and Males of Reproductive Potential: Pregnancy testing: Verify pregnancy status of females of reproductive potential prior to initiation of ENHERTU. Contraception: Females: ENHERTU can cause fetal harm when administered to a pregnant woman. Advise females of reproductive potential to use effective contraception during treatment with ENHERTU and for at least 7 months following the last dose. Males: Advise male patients with female partners of reproductive potential to use effective contraception during treatment with ENHERTU and for at least 4 months following the last dose. Infertility: ENHERTU may impair male reproductive function and fertility.
Pediatric Use: Safety and effectiveness of ENHERTU have not been established in pediatric patients.
Geriatric Use: Of the 234 patients with HER2-positive breast cancer treated with ENHERTU 5.4 mg/kg, 26% were ≥65 years and 5% were ≥75 years. No overall differences in efficacy were observed between patients ≥65 years of age compared to younger patients. There was a higher incidence of Grade 3-4 adverse reactions observed in patients aged ≥65 years (53%) as compared to younger patients (42%). Of the 125 patients with locally advanced or metastatic HER2‑positive gastric or GEJ adenocarcinoma treated with ENHERTU 6.4 mg/kg in DESTINY-Gastric01, 56% were ≥65 years and 14% were ≥75 years. No overall differences in efficacy or safety were observed between patients ≥65 years of age compared to younger patients.
Hepatic Impairment: In patients with moderate hepatic impairment, due to potentially increased exposure, closely monitor for increased toxicities related to the topoisomerase inhibitor.