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Zentalis Pharma to Begin ZN-c3 Combo Study in BRAF V600E-Mutant Colorectal Cancer

NEW YORK – Zentalis Pharmaceuticals on Monday said it began a Phase I/II trial of its Wee1 inhibitor ZN-c3 plus Pfizer's Braftovi (encorafenib) and Eli Lilly's Erbitux (cetuximab) in BRAF V600E-mutated metastatic colorectal cancer.

New York-based Zentalis is developing ZN-c3 in collaboration with Pfizer. Earlier this year, Pfizer made a $25 million equity investment in Zentalis to advance the firm's pipeline; the two firms also agreed to collaborate on the development of ZN-c3.

The Phase I/II trial of the ZN-c3 combination is expected to begin enrolling patients in Q1 2023. In 2020, Braftovi and Erbitux were approved by the US Food and Drug Administration for the treatment of BRAF V600E-mutant metastatic colorectal cancer.

"Combining ZN-c3 with [Braftovi and Erbitux] in this study represents an opportunity in our ZN-c3 clinical development program, alongside ongoing studies in both the monotherapy and chemotherapy combination settings in multiple tumor types," Zentalis Chief Medical Officer Carrie Brownstein said in a statement. "If successful in clinical trials and approved, the combination of ZN-c3 with targeted or DNA damage response agents could be another potential treatment option to help improve the lives of people living with BRAF-mutated metastatic colorectal cancer."

Zentalis is also studying ZN-c3 as a monotherapy in uterine cancer and solid tumors, as a combination treatment with chemo in ovarian cancer and osteosarcoma, and in combination with GlaxoSmithKline's Zejula (niraparib) in ovarian cancer.

Earlier this year, Zentalis also partnered with Caris Life Sciences to select patients for treatment with ZN-c3 in clinical trials.