Exelixis Announces Initiation of Phase 1 Trial Evaluating XL102 as a Single Agent and in Combination with Other Anti-Cancer Agents in Patients with Advanced or Metastatic Solid Tumors

Exelixis, Inc. (NASDAQ: EXEL) today announced initiation of the first-in-human phase 1 trial evaluating the safety, tolerability, pharmacokinetics and preliminary anti-tumor activity of XL102 alone or in combination with other anti-cancer agents in patients with inoperable locally advanced or metastatic solid tumors. XL102 is a potent, selective and orally bioavailable inhibitor of cyclin-dependent kinase 7 (CDK7), an important regulator of the cell cycle that has been implicated in cancer.

“The initiation of our first-in-human phase 1 trial of XL102 is an important step in our commitment to developing novel medicines that can help patients with cancer,” said Gisela Schwab, M.D., President, Product Development and Medical Affairs and Chief Medical Officer, Exelixis. “The potential of this novel CDK7 inhibitor has been shown in preclinical studies demonstrating anti-proliferative activity and an ability to induce cell death in multiple cancer cell lines. We are excited to begin this trial and look forward to the possibility of helping more patients with advanced or metastatic solid tumors.”

The XL102-101 trial is a phase 1, open-label dose-escalation and cohort-expansion study evaluating the safety, tolerability, pharmacokinetics, anti-tumor activity and effect on biomarkers of XL102 administered orally alone and in multiple combination regimens in up to 298 patients with advanced solid tumors. The study will include patients with advanced solid tumors for whom either life-prolonging therapies do not exist or available therapies are intolerable or no longer effective. It will begin with a dose-escalation stage to determine the maximum tolerated dose or recommended dose of XL102 as a single agent and in combination therapy. In the subsequent cohort-expansion stage, XL102 will be evaluated in patients with certain types of ovarian, breast and prostate cancers. The goal of the cohort-expansion stage is to evaluate the anti-tumor activity of XL102, as assessed per the Response Evaluation Criteria in Solid Tumors (RECIST) version 1.1, as well as its safety, tolerability and pharmacokinetic profile.

About XL102

XL102 is a potent, selective and orally bioavailable covalent inhibitor of CDK7, which is an important regulator of the cellular transcriptional and cell cycle machinery. CDK7 helps regulate cell cycle progression, with overexpression observed in multiple cancers, such as breast and gastric. In preclinical studies, XL102 revealed potent anti-proliferative activity, induced cell death in a large panel of cancer cell lines and caused tumor growth inhibition and regression in xenograft models, demonstrating its potential as a targeted antitumor agent.