New Publication Finds Combination of WP1066 and Radiation Resulted in Long-Term Survival in Human Brain Tumor Mouse Model

On July 1, 2020 Moleculin Biotech, Inc., (Nasdaq: MBRX) ("Moleculin" or the "Company"), a clinical stage pharmaceutical company with a broad portfolio of drug candidates targeting highly resistant tumors and viruses, reported that a peer-reviewed article published in Clinical Cancer Research (Clin Cancer Res June 30 2020 DOI:10.1158/1078-0432.CCR-19-4092) reported findings that Moleculin’s STAT3 inhibitor, WP1066, used in combination with traditional whole brain radiation therapy (WBRT) resulted in long-term survivors and enhanced median survival time relative to monotherapy in mice with implanted human brain tumors (Press release, Moleculin, JUL 1, 2020, View Source [SID1234561618]).

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The study was performed by lead author Martina Ott, Ph.D., Instructor of Neurosurgery, senior author Amy Heimberger, M.D., professor of Neurosurgery, and a team of researchers at The University of Texas MD Anderson Cancer Center. Heimberger also is the Principle Investigator of the current investigator-initiated clinical trial of WP1066 for brain tumors.

In the current study, C57BL/6 mice underwent intracerebral implantation of GL261 glioma cells, WBRT, and treatment with WP1066, a blood-brain barrier penetrant inhibitor of the STAT3 pathway, or the two in combination. The role of the immune system was evaluated using tumor rechallenge strategies, immune incompetent backgrounds, immunofluorescence, immune phenotyping of tumor-infiltrating immune cells (via flow cytometry), and nanostring gene expression analysis of 770 immune-related genes from immune cells, including those directly isolated from the tumor microenvironment.

The combination of WP1066 and WBRT resulted in long-term survivors and enhanced median survival time relative to monotherapy in the GL261 glioma model (combination vs. control p<0.0001). Immunological memory appeared to be induced, because mice were protected during subsequent tumor rechallenge. The therapeutic effect of the combination was completely lost in immune incompetent animals. Nanostring analysis and immunofluorescence revealed immunological reprograming in the brain tumor microenvironment specifically affecting dendritic-cell antigen presentation and T cell effector functions. The study indicates that the combination of STAT3 inhibition and WBRT enhances the therapeutic effect against gliomas in the CNS by inducing dendritic-cell and T cell interactions in the brain tumor, which seems to be a requirement for a fully functional immune response
"This impressive study confirms preliminary data we announced last year," commented Walter Klemp, Chairman and CEO of Moleculin. "Importantly, the study indicated that the combination of STAT3 inhibition with whole brain radiotherapy had the capacity to enhance the therapeutic effect against established tumors as well as developing immune memory that appears to prevent recurrence."

The research was supported by the Cancer Prevention & Research Institute of Texas (IIRA-RP160482), the National Institutes of Health (CA1208113, P50 CA093459, P50 CA127001 and P30 CA016672), the Ben and Catherine Ivy Foundation, MD Anderson’s Glioblastoma Moon Shot, and the Brockman Foundation.

Ipsen presents Phase I/II clinical data evaluating liposomal irinotecan (Onivyde®) as an investigational first-line combination treatment for metastatic pancreatic cancer at the ESMO World Congress on Gastrointestinal Cancer

On July 1, 2020 Ipsen (Euronext: IPN; ADR: IPSEY), reported the primary analysis of the Phase I/II study evaluating the investigational use of irinotecan liposome injection (Onivyde) in combination with 5-fluorouracil/leucovorin (5-FU/LV) and oxaliplatin (OX) together, known as NALIRIFOX in study patients with previously untreated, unresectable, locally advanced and metastatic pancreatic ductal adenocarcinoma (PDAC) during a late-breaking oral presentation at the ESMO (Free ESMO Whitepaper) World Congress on Gastrointestinal Cancer (WCGI), 1–5 July 2020 (Press release, Ipsen, JUL 1, 2020, View Source [SID1234561617]). The results include safety and efficacy analyses from the multicenter, open-label, study consisting of dose-exploration safety run-in (traditional 3+3 design) to confirm the maximum tolerated dose and appropriate dose regimen for NALIRIFOX in the dose-expansion phase.1

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No new safety signals were observed in the 32 patients evaluated from the recommended NALIRIFOX 50/60 mg/m2 dose (primary endpoint). Study patients achieved median progression-free survival of 9.2 months and median overall survival of 12.6 months (secondary endpoints).1

These data, in addition to promising anti-tumor activity highlighted by secondary endpoints, have led to the initiation of patient enrollment for the international Phase III NAPOLI-3 clinical study investigating the safety and efficacy of NALIRIFOX versus gemcitabine + nab-paclitaxel in the first-line setting.2 On 5 June 2020, Ipsen was granted Fast Track designation from the U.S. Food and Drug Administration (FDA) to facilitate the development and potentially expedite the review of NALIRIFOX in this indication. Programs with Fast Track designation may benefit from early and frequent interactions with the FDA over the course of drug development. In addition, the Fast Track designation program allows for the eligibility for accelerated approval and priority review if relevant study criteria are met and enables a company to submit individual sections of a New Drug Application (NDA) for review on a rolling-submission basis.

"Pancreatic cancer is aggressive, and we continue to investigate opportunities to improve outcomes for more patients that can extend survival. Unfortunately, current treatments, including immunotherapies that are transforming outcomes for patients with other solid tumors, have not demonstrated similar success in pancreatic cancer." said Zev Wainberg, M.D., lead investigator and associate professor of medicine, University of California Los Angeles. "The initial median progression-free and overall survival data from our Phase I/II trial are promising and we look forward to seeing how this investigational first-line treatment compares to gemcitabine + nab-paclitaxel in the Phase III trial now underway."

"A year following the read out of the preliminary Phase I/II study, we remain encouraged by the data, which demonstrated no new safety signals and continued to show anti-tumor activity," said Howard Mayer, M.D., Executive Vice President, Head of Research and Development at Ipsen. "Ipsen is committed to patients with pancreatic cancer. We are currently enrolling patients in our NAPOLI-3 Phase III clinical study across the U.S. and in other countries to gain a better understanding of the role of liposomal irinotecan as a potential first-line combination treatment for locally advanced and metastatic pancreatic cancer."

The Phase I/II, open-label trial (NCT02551991) was designed to assess the safety, tolerability and dose-limiting toxicities (DLTs) of NALIRIFOX for the first-line dosing of study participants with locally advanced and metastatic pancreatic cancer. Secondary objectives were to assess clinical efficacy, defined by median progression-free survival (PFS) and median overall survival (OS), best overall response rate, overall response rate (ORR), disease control rate at 16 weeks (DCR) and duration of response (DoR).1

The final analysis as of the data cut off on 26 February 2020 included all study participants from the pooled population (n=32: Part 1A-cohort B dose exploration phase n=7; Part 1B-dose expansion phase n=25) who received the maximum tolerated dose of liposomal irinotecan 50 mg/m2 [free-base], LV 400 mg/m2, 5-FU 2400 mg/m2, and OX 60 mg/m2). Patients were aged ≥ 18 years with an Eastern Cooperative Oncology Group (ECOG) performance status score ≤ 1 and adequate organ function.1 The preliminary results from this study were presented at the ESMO (Free ESMO Whitepaper) World Congress on Gastrointestinal Cancer in July 2019.

Phase I/II Safety Results1:

No reported Grade 3 or higher fatigue or peripheral neuropathy.
Treatment emergent adverse events (TEAEs) Grade 3 or higher were reported by 22 of 32 study patients and included: neutropenia (31.3%), febrile neutropenia (12.5%), hypokalemia (12.5%), anemia (12.5%), diarrhea (9.4%), nausea (9.4%) and decreased neutrophil count (9.4%); vomiting occurred in 6.3% of patients.
8 patients reported TEAEs leading to discontinuation of oxaliplatin alone or all four study drugs (n=8/32), with 26 study patients requiring dose adjustment due to AEs.

Phase I/II Efficacy Results1:

Study patients saw a median PFS (95% CI) of 9.2 months (7.69, 11.96) and median OS of 12.6 months (8.74, 18.69).
BOR (Best Overall Response) included: one complete response (CR; study participant diagnosed with locally advanced Stage III disease) in 3% (1/32), 10 partial responses (PR) in 31.3% (10/32) and 15 stable diseases (SD) in 46.9% (15/32) (sum of CR+PR+SD = 81.3%).
Disease control achieved by 71.9% (23/32) of study patients at 16 weeks.

ABOUT ONIVYDE (irinotecan liposome injection)

Ipsen has exclusive commercialization rights for the current and potential future indications for Onivyde in the U.S. Servier is responsible for the commercialization of Onivyde outside of the U.S. and Taiwan under an exclusive licensing agreement with Ipsen. PharmaEngine has commercial rights to Onivyde in Taiwan.

INDICATION – UNITED STATES

Onivyde is approved by the U.S. FDA in combination with fluorouracil (5-FU) and leucovorin (LV) for the treatment of patients with metastatic adenocarcinoma of the pancreas after disease progression following gemcitabine-based therapy. Limitation of Use: Onivyde is not indicated as a single agent for the treatment of patients with metastatic adenocarcinoma of the pancreas.

Please see full U.S. Prescribing Information and Boxed WARNING for ONIVYDE.

About the Phase I/II Study

The Phase I/II, open-label, comparative trial is designed to assess the safety, tolerability and dose-limiting toxicities of investigational irinotecan liposomal injection (Onivyde) in combination with 5-fluorouracil/leucovorin (5-FU/LV) and oxaliplatin (OX) as a potential first-line treatment for metastatic pancreatic ductal adenocarcinoma cancer patients. The study has enrolled 56 patients at 15 sites across the United States, Spain and Australia. It is being conducted in two parts:

Part 1a: a safety run-in as initial dose exploration
Part 1b: dose expansion of the liposomal irinotecan + 5-FU/LV + oxaliplatin regimen
The study’s primary endpoint is safety and tolerability. Secondary assessments of clinical efficacy include overall response rate, disease control rate and best overall response. For more information visit clinicaltrials.gov and use identifier NCT02551991.3

About the NAPOLI-3 Phase III Study

The NAPOLI-3 clinical trial is an open-label, randomized, multicenter, Phase III study of irinotecan liposome injection (Onivyde) in combination with oxaliplatin (OX) and 5-fluorouracil/leucovorin (5-FU/LV) versus nab-paclitaxel plus gemcitabine in subjects who have not previously received chemotherapy for metastatic adenocarcinoma of the pancreas. The purpose of this study is to look at the efficacy and safety of investigational irinotecan liposome injection in combination with other FDA-approved drugs used for cancer therapy compared to nab-paclitaxel + gemcitabine treatment in improving the overall survival of patients not previously treated for metastatic pancreatic cancer. The study’s primary endpoint is Overall survival (OS), with secondary outcome measures defined as Progression free survival (PFS) and Overall Response Rate (ORR).

Evelo Biosciences to Present Clinical Data from Phase 1/2 Trial of EDP1503 at the ESMO World Congress on Gastrointestinal Cancer Virtual Meeting

On July 1, 2020 Evelo Biosciences, Inc. (Nasdaq:EVLO), a clinical stage biotechnology company developing a new modality of orally delivered, systemically acting biologics, reported that clinical data from the Phase 1/2 open-label study of EDP1503, in combination with pembrolizumab, in patients with advanced metastatic microsatellite stable colorectal carcinoma (MSS CRC), triple-negative breast cancer (TNBC), and checkpoint inhibitor relapsed tumors, will be presented at the ESMO (Free ESMO Whitepaper) World Congress on Gastrointestinal Cancer Virtual Meeting being held July 1 – 4, 2020 (Press release, Evelo Biosciences, JUL 1, 2020, View Source [SID1234561615]).

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In addition to data in MSS CRC patients, the poster reported preliminary data on 11 TNBC patients (8 on high dose and 3 on low dose EDP1503). An overall response rate (ORR) of 25% (2/8) and a disease control rate of 37.5% (3/8) were observed across all TNBC subjects receiving high dose EDP1503. ORR was 33% (2/6) amongst response-evaluable patients on the high dose, with 2 patients awaiting first response assessment. Historic studies of anti-PD-1 monotherapy in heavily pretreated TNBC patients have yielded an ORR of 5-10%. The study continues enrollment in TNBC, and further data from this cohort will be available in 4Q 2020.

Details of the poster are as follows:

Title: EDP1503 induces antitumor responses via gut-mediated activation of both innate and adaptive immunity
Poster Session Date: July 1-4, 2020
Abstract ID: P-325
Category: Clinical Colon Cancer
Authors: Loise Francisco-Anderson, PhD; Shamira Shariffudin; Humphrey Gardner, MD; Michael Goldberg, PhD; Shubhra Kashyap, MS; Mary Abdou; Chris Davitt, PhD; Shannon Argueta, PhD; Pooja Parameswaran, MS; Peter Sandy, PhD; Holly Ponichtera, PhD; Mark Carlson; Maria Sizova, PhD; Valeria Kravitz; Erin Troy, PhD; Sam Andrewes, MS; Johanna C. Bendell, MD; Judy S. Wang, MD; Susanna V. Ulahannan, MD; Michael Chisamore, PhD; Mark Bodmer, PhD; and Duncan McHale, MD

The poster is available online on the ESMO (Free ESMO Whitepaper) conference website, as well as on the Evelo website, under the "publications" tab.

PRESS RELEASEBolt Biotherapeutics Closes $93.5 Million Series C Financing

On July 1, 2020 Bolt Biotherapeutics, Inc., a clinical-stage biotechnology company developing its Immune-Stimulating Antibody Conjugate (ISAC) platform technology to harness the power of the innate immune system to treat cancer, reported the closing of an oversubscribed $93.5 million Series C financing (Press release, Bolt Biotherapeutics, JUL 1, 2020, View Source [SID1234561613]). Led by Sofinnova Investments, the Series C financing included participation from new investors RA Capital Management, Surveyor Capital (a Citadel Company), Rock Springs Capital, Samsara BioCapital and Pfizer Ventures as well as existing investors Novo Holdings, Vivo Capital, Pivotal bioVenture Partners and others.

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Bolt is pioneering a new category of immunotherapies that combine the precision of antibody targeting with the power of the innate immune system via activating myeloid cells and reprogramming the tumor microenvironment. Bolt has raised more than $170 million since its founding in 2015, and this new round of funding will support the continued clinical development of its lead ISAC, BDC-1001, which is delivered systemically as monotherapy for HER2-expressing cancers. The financing will also support the expansion of the company’s pipeline of Boltbody therapeutics. Bolt’s expertise in myeloid biology lays the foundation for its innovative work developing proprietary innate immune stimulants for use in ISACs.

"The support from this marquee group of biotech investors is a testament to what we have recently accomplished, in particular the start of our first clinical trial for BDC-1001," said Randall Schatzman, Ph.D., the company’s chief executive officer. "We have built a strong team with expertise in key drug development areas, and this financing round will enable us to drive our ongoing clinical study and pipeline development work forward expeditiously. The Bolt technology has potential to significantly improve how we treat certain cancers and promises durable responses for patients. In addition to BDC1001, we are currently on track to nominate our next clinical candidates later this year."

In conjunction with the financing, Jason Pitts Ph.D., principal at Sofinnova Investments, will join the company’s board of directors. He states, "We believe Bolt is well-positioned to execute on its vision of developing immuno-oncology therapies with the potential to generate systemic immunological memory and provide durable clinical benefit. I look forward to helping the company realize their goal of developing the ISAC platform across a range of solid tumor targets."

Bolt is developing BDC-1001 as a monotherapy for patients with HER2-expressing solid tumors. The drug candidate is an ISAC comprised of trastuzumab conjugated to a Bolt proprietary TLR7/8 agonist payload. In preclinical models, systemic administration of HER2-ISACs demonstrate localized immune activation that results in robust single agent activity, generation of host immunological memory against cancer and epitope spreading. Preclinical data, which were presented at SITC (Free SITC Whitepaper) 2019, demonstrated complete, durable regression of established tumors resistant to trastuzumab and immunological memory providing protection against tumor cells that no longer express the HER2 antigen in syngeneic mouse cancer models. This offers the potential for durable and meaningful responses for HER2-expressing cancers.

Blueprint Medicines Announces Submission of New Drug Application to FDA for Pralsetinib for the Treatment of Advanced RET Mutant and RET Fusion-Positive Thyroid Cancers

On July 1, 2020 Blueprint Medicines Corporation (NASDAQ: BPMC), a precision therapy company focused on genomically defined cancers, rare diseases and cancer immunotherapy, reported the submission of a New Drug Application (NDA) to the U.S. Food and Drug Administration (FDA) for pralsetinib for the treatment of patients with advanced or metastatic RET mutant medullary thyroid cancer (MTC) and RET fusion-positive thyroid cancers (Press release, Blueprint Medicines, JUL 1, 2020, View Source [SID1234561612]). Pralsetinib is an investigational, once-daily precision therapy designed to potently and selectively inhibit RET fusions and mutations, including predicted resistance mutations.

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Blueprint Medicines submitted the NDA under the Real-Time Oncology Review pilot program (RTOR program), an initiative of the FDA’s Oncology Center of Excellence. The RTOR program aims to explore a more efficient review process to ensure that safe and effective treatments are available to patients as early as possible, while maintaining and improving review quality by the FDA.

"Pralsetinib has broad potential to address the medical needs of patients with RET-altered cancers, who have not traditionally benefited from targeted therapy even though their tumors have a known disease driver," said Andy Boral, M.D., Ph.D., Chief Medical Officer at Blueprint Medicines. "There are now pending marketing applications for pralsetinib in RET-altered non-small cell lung cancer and thyroid cancers, supporting our goal to advance treatment standards for these patients. We are working closely with the FDA and aim to bring this promising treatment to patients as expeditiously as possible."

In May 2020, Blueprint Medicines announced that the U.S. and EU marketing applications for pralsetinib for the treatment of locally advanced or metastatic RET fusion-positive non-small cell lung cancer (NSCLC) were accepted by the FDA and validated by the European Medicines Agency, respectively.

About RET-Altered Solid Tumors

RET activating fusions and mutations are key disease drivers in many cancer types, including NSCLC and MTC. RET fusions are implicated in approximately 1 to 2 percent of patients with NSCLC and approximately 10 to 20 percent of patients with papillary thyroid cancer, while RET mutations are implicated in approximately 90 percent of patients with advanced MTC. In addition, oncogenic RET alterations are observed at low frequencies in colorectal, breast, pancreatic and other cancers, and RET fusions have been observed in patients with treatment-resistant EGFR-mutant NSCLC.

About Pralsetinib

Pralsetinib is an investigational, once-daily oral precision therapy specifically designed for highly potent and selective targeting of oncogenic RET alterations. Blueprint Medicines is developing pralsetinib for the treatment of patients with RET-altered NSCLC, thyroid cancer and other solid tumors. The FDA has granted Breakthrough Therapy Designation to pralsetinib for the treatment of RET fusion-positive NSCLC that has progressed following platinum-based chemotherapy, and RET mutation-positive MTC that requires systemic treatment and for which there are no acceptable alternative treatments.

Pralsetinib was designed by Blueprint Medicines’ research team, leveraging the company’s proprietary compound library. In preclinical studies, pralsetinib consistently demonstrated sub-nanomolar potency against the most common RET fusions, activating mutations and predicted resistance mutations. In addition, pralsetinib demonstrated markedly improved selectivity for RET compared to pharmacologically relevant kinases, including approximately 80-fold improved potency for RET versus VEGFR2. By suppressing primary and secondary mutants, pralsetinib has the potential to overcome and prevent the emergence of clinical resistance. Blueprint Medicines believes this approach will enable durable clinical responses across a diverse range of RET alterations, with a favorable safety profile.

Blueprint Medicines has an exclusive collaboration and license agreement with CStone Pharmaceuticals for the development and commercialization of pralsetinib and certain other drug candidates in Mainland China, Hong Kong, Macau and Taiwan. Blueprint Medicines retains development and commercial rights for pralsetinib in the rest of the world.