zamzetoclax (GS-9716) / Gilead - LARVOL DELTA

Gilead culls…2 cancer assets (FierceBiotech) - "After the recent approval and launch of twice-yearly HIV prophylactic Yeztugo, Gilead is cleaning up its R&D pipeline. The Bay Area company has dropped two early-stage cancer candidates....The two culled oncology assets are a DGKα inhibitor called GS-9911 and an MCL1 inhibitor called zamzetoclax or GS-9716, according to an Aug. 7 earnings presentation. Both were being tested out in phase 1 trials, with GS-9911 being tested alone and in combination with an anti-PD-1 monoclonal antibody in patients with advanced solid tumors, and zamzetoclax alone or with other chemotherapies in patients with advanced solid malignancies. Gilead did not respond to Fierce Biotech's questions about the current status of the trials."

Pipeline update • Solid Tumor

Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of GS-9716 as Monotherapy and in Combination With Anticancer Therapies in Adults With Solid Malignancies (clinicaltrials.gov) - P1 | N=145 | Active, not recruiting | Sponsor: Gilead Sciences | Recruiting ➔ Active, not recruiting

Enrollment closed • Oncology • Solid Tumor

Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of GS-9716 as Monotherapy and in Combination With Anticancer Therapies in Adults With Solid Malignancies (clinicaltrials.gov) - P1 | N=145 | Recruiting | Sponsor: Gilead Sciences | Trial completion date: Jan 2027 ➔ Mar 2029 | Trial primary completion date: Jan 2027 ➔ Mar 2029

Monotherapy • Trial completion date • Trial primary completion date • Oncology • Solid Tumor

Potential biomarkers for MCL1 inhibitor sensitivity. (PubMed, Cell Signal (Middlet)) - "Currently, the MCL1 inhibitor GS-9716 is in clinical trials for TNBC therapy. If validated in clinical samples, this GS could potentially serve as a predictive biomarker for therapy response and help guide the selection of combination therapies to enhance the effectiveness of MCL1 inhibitors."

Biomarker • IO biomarker • Journal • Breast Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer • BCL2

Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of GS-9716 as Monotherapy and in Combination With Anticancer Therapies in Adults With Solid Malignancies (clinicaltrials.gov) - P1 | N=195 | Recruiting | Sponsor: Gilead Sciences

Combination therapy • Monotherapy • Trial completion date • Trial primary completion date • Oncology • Solid Tumor

Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of GS-9716 as Monotherapy and in Combination With Anticancer Therapies in Adults With Solid Malignancies (clinicaltrials.gov) - P1 | N=195 | Recruiting | Sponsor: Gilead Sciences | Trial completion date: May 2028 ➔ Jan 2027

Combination therapy • Monotherapy • Trial completion date • Oncology • Solid Tumor

GS-9716: A potent, selective and orally bioavailable small molecule inhibitor of MCL1 for the treatment of cancer (AACR 2022) - P1 | "In addition to single agent activity, GS-9716 showed strong synergy with multiple anti-cancer therapies; robust in vitro synergy was observed with venetoclax in the AML models and as well as with paclitaxel in the TNBC models. Similar responses were also observed when GS-9716 was dosed with paclitaxel in the TNBC PDX models. GS-9716 is currently in Phase 1 clinical trial evaluating safety, tolerability and pharmacokinetics as monotherapy and in combination with anticancer therapies in adults with advanced solid tumors (NCT05006794)."

IO biomarker • Acute Myelogenous Leukemia • Breast Cancer • Hematological Malignancies • Multiple Myeloma • Oncology • Solid Tumor • Triple Negative Breast Cancer • BCL2 • MCL1

Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of GS-9716 as Monotherapy and in Combination With Anticancer Therapies in Adults With Solid Malignancies (clinicaltrials.gov) - P1; N=205; Recruiting; Sponsor: Gilead Sciences; Not yet recruiting ➔ Recruiting

Clinical • Combination therapy • Enrollment open • Monotherapy • Breast Cancer • Endometrial Cancer • Esophageal Cancer • Gastric Cancer • Gastroesophageal Junction Adenocarcinoma • Gastrointestinal Cancer • Head and Neck Cancer • Hepatocellular Cancer • Immune Modulation • Lung Cancer • Lung Non-Squamous Non-Small Cell Cancer • Non Small Cell Lung Cancer • Oncology • Ovarian Cancer • Renal Cell Carcinoma • Solid Tumor • Thyroid Gland Carcinoma • Thyroid Gland Follicular Carcinoma • Triple Negative Breast Cancer • MRI