Pfizer and IDEAYA Enter Clinical Collaboration to Develop Combination Therapy Targeting GNAQ/GNA11-Mutant Solid Tumors

On the 19th, IDEAYA Biosciences announced that it has entered into a clinical research and development collaboration agreement with Pfizer to evaluate the efficacy of the combination of IDEAYA’s investigational small-molecule protein kinase C (PKC) inhibitor IDE196 and Pfizer’s MEK inhibitor binimetinib in patients with solid tumors harboring GNAQ or GNA11 mutations, including those with metastatic uveal melanoma (MUM), cutaneous melanoma, and colorectal cancer (CRC).

IDE196, developed by IDEAYA Biosciences, is a small-molecule inhibitor targeting PKC. The PKC protein kinase family is located upstream of the MEK/MAPK signaling pathway and downstream of the G protein signaling pathway. PKC participates in signal transduction that influences cell proliferation or transcriptional regulation. Either upstream gene mutations in GNAQ or GNA11, or PRKC gene fusions, can lead to constitutive activation of PKC, thereby inducing cancer.

IDEAYA and Pfizer will establish a Joint Development Committee (JDC), through which both parties will make joint decisions and share data regarding clinical trial results. IDEAYA will sponsor the study, and Pfizer will provide binimetinib for the research. The study will evaluate the response rate, efficacy, and durability of inhibiting the MAP kinase signaling pathway at two nodes—upstream PKC and downstream MEK—in patients with solid tumors harboring GNAQ or GNA11 gene mutations. Furthermore, the clinical trial will investigate the pharmacokinetics of each drug and the tolerability of the combination therapy. The trial is expected to commence in mid-2020.

▲Schematic diagram of the mechanism of action of IDE196 (Image source: IDEAYA official website)

“There are approximately 6,000 patients with MUM, cutaneous melanoma, CRC, and other solid tumors harboring GNAQ or GNA11 gene mutations in the United States and the five major European countries, and currently no approved targeted therapies for this genetic mutation are available,” said Mr. Yujiro S. Hata, Chief Executive Officer and President of IDEAYA Biosciences. “We look forward to evaluating the clinical potential of binimetinib in combination with IDE196 in this patient population.”

References:

[1] IDEAYA and Pfizer Enter Clinical Trial Collaboration and Supply Agreement to Evaluate Clinical Combination of IDE196 and Binimetinib in Solid Tumors Harboring GNAQ or GNA11 Hotspot Mutations, Retrieved March 18, 2020, from https://ir.ideayabio.com/news-releases/news-release-details/ideaya-and-pfizer-enter-clinical-trial-collaboration-and-supply

Original Title: Flash | Pfizer and IDEAYA Biosciences Partner to Develop Tumor-Agnostic Anticancer Therapy Combinations

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