Bold Therapeutics Successfully Initiates Clinical Trial of First-in-Class Anti-Cancer Agent BOLD-100

On October 9, 2020 Bold Therapeutics, a clinical-stage biopharmaceutical company, reported that the first patient for the company’s Phase 1b oncology clinical trial has been enrolled at the Cross Cancer Institute (Edmonton, Alberta) under Principal Investigator Dr. Jennifer Spratlin (Press release, Bold Therapeutics, OCT 9, 2020, View Source [SID1234568272]). This trial investigates the safety and tolerability of Bold Therapeutics’ first-in-class anti-cancer agent, BOLD-100, in combination with the current standard-of-care, FOLFOX (5-fluorouracil, leucovorin, oxaliplatin), for the treatment of patients with advanced gastric, pancreatic, colorectal and bile duct cancers. Five additional hospitals across Canada will also be enrolling patients: Princess Margaret Cancer Centre in Toronto, Ontario (PI Grainne O’Kane); Ottawa General Hospital in Ottawa, Ontario (PI Rachel Goodwin); Juravinski Cancer Centre in Hamilton, Ontario (PI Elaine McWhirter); and Jewish General Hospital and Royal Victoria Hospital in Montreal, Quebec (PIs Petr Kavan and Jamil Asselah, respectively).

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BOLD-100 is a first-in-class ruthenium-based therapeutic that selectively inhibits stress-induced upregulation of GRP78 and alters the unfolded protein response (UPR), mitigating resistance, survival and proliferation, with additional synergistic direct anti-cancer activity.

"Bold Therapeutics has achieved another key clinical development milestone. The current trial will provide data on not only the safety and tolerability of BOLD-100 in combination with FOLFOX, but also important efficacy measures to evaluate patient outcomes," stated Jim Pankovich, EVP of Clinical Development. "Bold Therapeutics is working with an experienced team of investigators across Canada – and, later, in the United States and South Korea – for this groundbreaking clinical trial. The dose-escalation portion of this adaptive-design study will enroll approximately 12 patients in cohorts of three after which the expansion-cohort portion will enroll up to 80 patients, with 20 patients in each arm."

In a previously completed 46-patient Phase 1 monotherapy study, BOLD-100 was well-tolerated with minimal hematological and neurological side effects, suggesting it could be combined favorably with other anti-cancer therapies. Preclinical data shows profound synergy in combination with numerous drug classes ranging from traditional chemotherapies to newer targeted therapies and immuno-oncology agents. The company received a No Objection Letter (NOL) from Health Canada earlier this year and has an open Investigational New Drug (IND) and an Orphan Drug Designation (ODD) in pancreatic cancer in the United States, with additional ODDs expected over the next six months.

"Cancer drug resistance remains a significant challenge for patients and physicians. We have deliberately chosen some of the most difficult-to-treat indications with the shortest mean survival times for this trial because this is where there is the greatest unmet medical need," said E. Russell McAllister, CEO. "Preclinically, BOLD-100 significantly improves outcomes in a wide range of different indications and combinations, acting through both anti-resistance but also direct anti-cancer pathways. We are now actively evaluating additional development options, some in partnership with other pharmaceutical companies, and we expect to initiate at least one additional oncology clinical trial in 2021. Areas of particular interest include triple-negative breast cancer; neoadjuvant therapy; first-line combinations with immuno-oncology agents; sarcomas; and various liquid tumors, including multiple myeloma – all of which are potentially viable development indications and combinations based on preclinical data and/or relevant literature."

PENELOPE-B Trial of IBRANCE® (palbociclib) in Early Breast Cancer Did Not Meet Primary Endpoint

On October 9, 2020 The German Breast Group (GBG) and Pfizer Inc. (NYSE: PFE) reported that the collaborative Phase 3 PENELOPE-B trial did not meet the primary endpoint of improved invasive disease-free survival (iDFS) in women with hormone receptor-positive (HR+), human epidermal growth factor-negative (HER2-) early breast cancer (eBC) who have residual invasive disease after completing neoadjuvant chemotherapy. No unexpected safety signals were observed (Press release, Pfizer, OCT 9, 2020, View Source [SID1234568271]).

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PENELOPE-B is a randomized, double-blind, placebo-controlled Phase 3 study comparing one year of palbociclib plus at least five years of standard adjuvant endocrine therapy to placebo plus at least five years of standard adjuvant endocrine therapy. The trial is sponsored by the GBG as part of a clinical research collaboration with Pfizer and other study groups.

"Reducing the risk of disease recurrence in patients who have residual disease after neoadjuvant chemotherapy is a complex clinical challenge," said Professor Sibylle Loibl, Chair of GBG. "This unique trial was made possible through the collaboration and support from all the research partners involved. Despite this outcome, we believe that key learnings will emerge from the large number of biomarkers being analyzed from collected tumor tissue, which will help inform future breast cancer research."

"This is the first randomized Phase 3 study to establish mature iDFS results for a CDK4/6 inhibitor as part of the adjuvant treatment for early breast cancer. While we are disappointed with this result, we look forward to continuing to work with our research partners to understand subgroup data and how these could inform the development of our next-generation CDK inhibitors in early breast cancer," said Chris Boshoff, M.D., Ph.D., Chief Development Officer, Oncology, Pfizer Global Product Development. "We are proud of the transformative impact IBRANCE has had on the treatment of HR+, HER2- metastatic breast cancer – a vastly different treatment setting than early breast cancer. Our commitment to the metastatic patient community is as strong as ever as we continue to generate new data, including the most extensive body of real-world evidence for a CDK 4/6 inhibitor."

Detailed findings from PENELOPE-B will be presented at an upcoming medical congress.

About the PENELOPE-B Study

PENELOPE-B is a randomized, double-blind, placebo-controlled Phase 3 study comparing one year of palbociclib plus at least five years of standard adjuvant endocrine therapy to placebo plus at least five years of standard adjuvant endocrine therapy in 1,250 women with HR+, HER2- eBC at high risk of recurrence who have residual invasive disease after completing neoadjuvant chemotherapy. Patients in the trial scored 3 or higher (or 2 if there were lymph node metastases at the time of surgery) on the clinical-pathologic stage – estrogen/grade (CPS-EG). The CPS-EG is a validated risk assessment tool combining: clinical stage before neoadjuvant treatment, pathological stage after neoadjuvant treatment, grading and estrogen-receptor status. The trial is sponsored by the GBG as part of a clinical research collaboration with other study groups, including ABCSG, AGO-B, ANZBCTG, BIG, CCTG, GEICAM, LACOG, IBCSG, ICORG, ISPy-2, JBCRG, KCSG, NSABP, Unicancer and Pfizer.

More than 190 clinical sites in 12 countries around the globe participated in PENELOPE-B. The study opened in November 2013 and closed recruitment on December 31, 2017.

About IBRANCE (palbociclib) 125 mg tablets and capsules

IBRANCE is an oral inhibitor of CDKs 4 and 6,1 which are key regulators of the cell cycle that trigger cellular progression.2,3 In the U.S., IBRANCE is indicated for the treatment of adult patients with HR+, HER2- advanced or metastatic breast cancer in combination with an aromatase inhibitor as initial endocrine based therapy in postmenopausal women or in men; or with fulvestrant in patients with disease progression following endocrine therapy.

IBRANCE currently is approved in more than 95 countries and has been prescribed to nearly 340,000 patients globally. IBRANCE is not indicated for early breast cancer.

The full U.S. Prescribing Information for the IBRANCE tablets and the IBRANCE capsules can be found here and here.

IMPORTANT IBRANCE (palbociclib) SAFETY INFORMATION FROM THE U.S. PRESCRIBING INFORMATION

Neutropenia was the most frequently reported adverse reaction in PALOMA-2 (80%) and PALOMA-3 (83%). In PALOMA-2, Grade 3 (56%) or 4 (10%) decreased neutrophil counts were reported in patients receiving IBRANCE plus letrozole. In PALOMA-3, Grade 3 (55%) or Grade 4 (11%) decreased neutrophil counts were reported in patients receiving IBRANCE plus fulvestrant. Febrile neutropenia has been reported in 1.8% of patients exposed to IBRANCE across PALOMA-2 and PALOMA-3. One death due to neutropenic sepsis was observed in PALOMA-3. Inform patients to promptly report any fever.

Monitor complete blood count prior to starting IBRANCE, at the beginning of each cycle, on Day 15 of first 2 cycles and as clinically indicated. Dose interruption, dose reduction, or delay in starting treatment cycles is recommended for patients who develop Grade 3 or 4 neutropenia.

Severe, life-threatening, or fatal interstitial lung disease (ILD) and/or pneumonitis can occur in patients treated with CDK4/6 inhibitors, including IBRANCE when taken in combination with endocrine therapy. Across clinical trials (PALOMA-1, PALOMA-2, PALOMA-3), 1.0% of IBRANCE-treated patients had ILD/pneumonitis of any grade, 0.1% had Grade 3 or 4, and no fatal cases were reported. Additional cases of ILD/pneumonitis have been observed in the post-marketing setting, with fatalities reported.

Monitor patients for pulmonary symptoms indicative of ILD/pneumonitis (e.g. hypoxia, cough, dyspnea). In patients who have new or worsening respiratory symptoms and are suspected to have developed pneumonitis, interrupt IBRANCE immediately and evaluate the patient. Permanently discontinue IBRANCE in patients with severe ILD or pneumonitis.

Based on the mechanism of action, IBRANCE can cause fetal harm. Advise females of reproductive potential to use effective contraception during IBRANCE treatment and for at least 3 weeks after the last dose. IBRANCE may impair fertility in males and has the potential to cause genotoxicity. Advise male patients to consider sperm preservation before taking IBRANCE. Advise male patients with female partners of reproductive potential to use effective contraception during IBRANCE treatment and for 3 months after the last dose. Advise females to inform their healthcare provider of a known or suspected pregnancy. Advise women not to breastfeed during IBRANCE treatment and for 3 weeks after the last dose because of the potential for serious adverse reactions in nursing infants.

The most common adverse reactions (≥10%) of any grade reported in PALOMA-2 for IBRANCE plus letrozole vs placebo plus letrozole were neutropenia (80% vs 6%), infections (60% vs 42%), leukopenia (39% vs 2%), fatigue (37% vs 28%), nausea (35% vs 26%), alopecia (33% vs 16%), stomatitis (30% vs 14%), diarrhea (26% vs 19%), anemia (24% vs 9%), rash (18% vs 12%), asthenia (17% vs 12%), thrombocytopenia (16% vs 1%), vomiting (16% vs 17%), decreased appetite (15% vs 9%), dry skin (12% vs 6%), pyrexia (12% vs 9%), and dysgeusia (10% vs 5%).

The most frequently reported Grade ≥3 adverse reactions (≥5%) in PALOMA-2 for IBRANCE plus letrozole vs placebo plus letrozole were neutropenia (66% vs 2%), leukopenia (25% vs 0%), infections (7% vs 3%), and anemia (5% vs 2%).

Lab abnormalities of any grade occurring in PALOMA-2 for IBRANCE plus letrozole vs placebo plus letrozole were decreased WBC (97% vs 25%), decreased neutrophils (95% vs 20%), anemia (78% vs 42%), decreased platelets (63% vs 14%), increased aspartate aminotransferase (52% vs 34%), and increased alanine aminotransferase (43% vs 30%).

The most common adverse reactions (≥10%) of any grade reported in PALOMA-3 for IBRANCE plus fulvestrant vs placebo plus fulvestrant were neutropenia (83% vs 4%), leukopenia (53% vs 5%), infections (47% vs 31%), fatigue (41% vs 29%), nausea (34% vs 28%), anemia (30% vs 13%), stomatitis (28% vs 13%), diarrhea (24% vs 19%), thrombocytopenia (23% vs 0%), vomiting (19% vs 15%), alopecia (18% vs 6%), rash (17% vs 6%), decreased appetite (16% vs 8%), and pyrexia (13% vs 5%).

The most frequently reported Grade ≥3 adverse reactions (≥5%) in PALOMA-3 for IBRANCE plus fulvestrant vs placebo plus fulvestrant were neutropenia (66% vs 1%) and leukopenia (31% vs 2%).

Lab abnormalities of any grade occurring in PALOMA-3 for IBRANCE plus fulvestrant vs placebo plus fulvestrant were decreased WBC (99% vs 26%), decreased neutrophils (96% vs 14%), anemia (78% vs 40%), decreased platelets (62% vs 10%), increased aspartate aminotransferase (43% vs 48%), and increased alanine aminotransferase (36% vs 34%).

Avoid concurrent use of strong CYP3A inhibitors. If patients must be administered a strong CYP3A inhibitor, reduce the IBRANCE dose to 75 mg. If the strong inhibitor is discontinued, increase the IBRANCE dose (after 3-5 half-lives of the inhibitor) to the dose used prior to the initiation of the strong CYP3A inhibitor. Grapefruit or grapefruit juice may increase plasma concentrations of IBRANCE and should be avoided. Avoid concomitant use of strong CYP3A inducers. The dose of sensitive CYP3A substrates with a narrow therapeutic index may need to be reduced as IBRANCE may increase their exposure.

For patients with severe hepatic impairment (Child-Pugh class C), the recommended dose of IBRANCE is 75 mg. The pharmacokinetics of IBRANCE have not been studied in patients requiring hemodialysis.

ADC Therapeutics Announces Full Exercise of Underwriters’ Option to Purchase Additional Common Shares

On October 9, 2020 ADC Therapeutics SA (NYSE: ADCT), a late clinical-stage oncology-focused biotechnology company pioneering the development and commercialization of highly potent and targeted antibody drug conjugates for patients with hematological malignancies and solid tumors, reported the underwriters in its recent upsized public offering of 6,000,000 common shares, which closed on September 28, 2020, have exercised in full their option to purchase an additional 900,000 common shares from the selling shareholders at the public offering price of $34.00 per share, less underwriting discounts and commissions (Press release, ADC Therapeutics, OCT 9, 2020, View Source [SID1234568270]). ADC Therapeutics did not receive any proceeds from the sale of shares by the selling shareholders.

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Morgan Stanley, BofA Securities and Cowen acted as joint book-running managers for the offering. RBC Capital Markets acted as co-manager for the offering.

The offering is being made only by means of a prospectus. Copies of the prospectus relating to the offering may be obtained from Morgan Stanley & Co. LLC, Attn: Prospectus Department, 180 Varick Street, 2nd Floor, New York, NY 10014 or by email at [email protected]; BofA Securities, Inc., NC1-004-03-43, 200 North College Street, 3rd floor, Charlotte, NC 28255-0001, Attn: Prospectus Department, or by email at [email protected]; or Cowen and Company, LLC, c/o Broadridge Financial Solutions, Attn: Prospectus Department, 1155 Long Island Avenue, Edgewood, NY 11717, by telephone at (833) 297-2926 or by email at [email protected].

A registration statement relating to these securities has been filed with, and declared effective by, the U.S. Securities and Exchange Commission. This press release shall not constitute an offer to sell or the solicitation of an offer to buy these securities, nor shall there be any sale of these securities in any state or jurisdiction in which such offer, solicitation or sale would be unlawful prior to registration or qualification under the securities laws of any such state or jurisdiction. There is no intention or permission to publicly offer, solicit, sell or advertise, directly or indirectly, any securities of ADC Therapeutics SA, such as the common shares, in or into Switzerland within the meaning of the Swiss Financial Services Act ("FinSA") and these securities will not be listed or admitted to trading on the SIX Swiss Exchange or on any other regulated trading venue (exchange or multilateral trading facility) in Switzerland. Neither this document nor any other offering or marketing material relating to these securities, such as the common shares, constitutes or will constitute a prospectus pursuant to the FinSA, and neither this document nor any other offering or marketing material relating to the common shares constitutes a prospectus pursuant to the FinSA, and neither this document nor any other offering or marketing material relating to the common shares may be publicly distributed or otherwise made publicly available in Switzerland.

Exelixis to Present the Preclinical Profile and Initial Clinical Pharmacokinetics of XL092, Its Next-Generation Oral Tyrosine Kinase Inhibitor

On October 9, 2020 Exelixis, Inc. (NASDAQ: EXEL) reported new data that support the ongoing clinical development of XL092, the company’s next-generation oral tyrosine kinase inhibitor that targets VEGF receptors, MET, AXL, MER, and other kinases implicated in cancer’s growth and spread (Press release, Exelixis, OCT 9, 2020, View Source [SID1234568268]). The new data will be presented in a poster discussion session (Abstract 33) as part of the 32nd EORTC-NCI-AACR (Free EORTC-NCI-AACR Whitepaper) (ENA) Symposium, which is being held virtually October 24-25; abstracts for the meeting were released earlier today.

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"When the XL092 program began, we wanted to develop a novel tyrosine kinase inhibitor that retained the target profile of cabozantinib, our flagship medicine that is now a global oncology franchise, while also improving on certain important characteristics"

"When the XL092 program began, we wanted to develop a novel tyrosine kinase inhibitor that retained the target profile of cabozantinib, our flagship medicine that is now a global oncology franchise, while also improving on certain important characteristics," said Peter Lamb, Ph.D., Executive Vice President of Scientific Strategy and Chief Scientific Officer of Exelixis. "The data to be presented at the ENA Symposium suggest XL092 has a desirable therapeutic profile that pairs the potential for significant anti-tumor activity with a much shorter clinical half-life than cabozantinib. The data also support a potential synergistic effect for XL092 in combination with immune checkpoint inhibitors, which is why we’re excited to expand our ongoing phase 1 clinical trial to include an exploration of the combination of XL092 and atezolizumab in multiple solid tumors."

The abstract released today provides a summary of results from a detailed characterization of XL092 in cancer cell lines and animal tumor models, as well as initial PK data from the ongoing phase 1 trial of the compound. Additional data will be presented in the poster discussion, which is scheduled to begin at 22:40 CEST / 4:40 p.m. EDT / 1:40 p.m. PDT on Saturday, October 24. Key findings included in the abstract are:

XL092 is an ATP-competitive inhibitor of multiple receptor tyrosine kinases including MET, VEGFR2, AXL and MER, with IC50 values in cell-based assays of 15, 1.6, 3.4, and 7.2 nM, respectively.
In xenograft studies, XL092 caused substantial tumor growth inhibition following 10 mg/kg daily oral dosing for 14 days, which was accompanied by significant inhibition of MET, AXL and VEGFR2 phosphorylation.
When XL092 was combined with an immune checkpoint inhibitor (ICI) in a syngeneic tumor model, the combination was significantly more efficacious than either XL092 or anti-PD1 alone.
PK data from the ongoing phase 1 clinical trial assessing daily dosing of XL092 in patients with advanced solid tumors shows a terminal half-life of 24 hours versus a 99-hour terminal half-life for cabozantinib.
The ongoing phase 1 trial (NCT03845166) is a multi-center study designed to evaluate the pharmacokinetics, safety, tolerability, and preliminary anti-tumor activity of XL092, both as a single agent and in combination with ICIs. The study protocol was recently amended to include dose-escalation and expansion cohorts for XL092 in combination with the ICI atezolizumab (TECENTRIQ). The dose-escalation evaluation of XL092 as a single agent is ongoing, and Exelixis anticipates patient enrollment in the dose-escalation evaluation of the combination regimen imminently. As recommended doses of single-agent XL092 and XL092 in combination with atezolizumab are established, the trial will proceed to enroll expansion cohorts in patients with clear cell and non-clear cell renal cell carcinoma, hormone-receptor positive breast cancer, and metastatic castration-resistant prostate cancer.

About XL092

XL092 is a next-generation oral tyrosine kinase inhibitor that targets VEGF receptors, MET, AXL, MER, and other kinases implicated in cancer’s growth and spread. In designing XL092, Exelixis sought to build upon the experience and target profile of cabozantinib, the company’s flagship medicine, while improving key characteristics, including clinical half-life. The compound is the subject of an ongoing phase 1 trial (NCT03845166) evaluating its pharmacokinetics, safety, tolerability, and preliminary anti-tumor activity when administered alone and in combination with the ICI atezolizumab (TECENTRIQ); pending positive data, further development is planned.

ADC Therapeutics Announces Full Exercise of Underwriters’ Option to Purchase Additional Common Shares

On October 9, 2020 ADC Therapeutics SA (NYSE: ADCT), a late clinical-stage oncology-focused biotechnology company pioneering the development and commercialization of highly potent and targeted antibody drug conjugates for patients with hematological malignancies and solid tumors, reported the underwriters in its recent upsized public offering of 6,000,000 common shares, which closed on September 28, 2020, have exercised in full their option to purchase an additional 900,000 common shares from the selling shareholders at the public offering price of $34.00 per share, less underwriting discounts and commissions (Press release, ADC Therapeutics, OCT 9, 2020, View Source [SID1234568265]). ADC Therapeutics did not receive any proceeds from the sale of shares by the selling shareholders.

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Morgan Stanley, BofA Securities and Cowen acted as joint book-running managers for the offering. RBC Capital Markets acted as co-manager for the offering.

The offering is being made only by means of a prospectus. Copies of the prospectus relating to the offering may be obtained from Morgan Stanley & Co. LLC, Attn: Prospectus Department, 180 Varick Street, 2nd Floor, New York, NY 10014 or by email at [email protected]; BofA Securities, Inc., NC1-004-03-43, 200 North College Street, 3rd floor, Charlotte, NC 28255-0001, Attn: Prospectus Department, or by email at [email protected]; or Cowen and Company, LLC, c/o Broadridge Financial Solutions, Attn: Prospectus Department, 1155 Long Island Avenue, Edgewood, NY 11717, by telephone at (833) 297-2926 or by email at [email protected].

A registration statement relating to these securities has been filed with, and declared effective by, the U.S. Securities and Exchange Commission. This press release shall not constitute an offer to sell or the solicitation of an offer to buy these securities, nor shall there be any sale of these securities in any state or jurisdiction in which such offer, solicitation or sale would be unlawful prior to registration or qualification under the securities laws of any such state or jurisdiction. There is no intention or permission to publicly offer, solicit, sell or advertise, directly or indirectly, any securities of ADC Therapeutics SA, such as the common shares, in or into Switzerland within the meaning of the Swiss Financial Services Act ("FinSA") and these securities will not be listed or admitted to trading on the SIX Swiss Exchange or on any other regulated trading venue (exchange or multilateral trading facility) in Switzerland. Neither this document nor any other offering or marketing material relating to these securities, such as the common shares, constitutes or will constitute a prospectus pursuant to the FinSA, and neither this document nor any other offering or marketing material relating to the common shares constitutes a prospectus pursuant to the FinSA, and neither this document nor any other offering or marketing material relating to the common shares may be publicly distributed or otherwise made publicly available in Switzerland.