NEW YORK--(BUSINESS WIRE)-- AnHeart Therapeutics (“AnHeart”), a clinical-stage global biopharmaceutical company committed to developing novel cancer therapies, today announced that the first patient has been dosed in the global Phase 2 trial of taletrectinib in ROS1 fusion-positive lung cancer (TRUST-II). Taletrectinib, the company’s lead candidate, is an investigational next-generation tyrosine kinase inhibitor (TKI) designed to effectively target ROS1 and NTRK fusion mutations.

ROS1 rearrangement is estimated to be an oncogenic driver in approximately 2 to 3 percent of patients with advanced NSCLC, and NTRK rearrangement is estimated to be an oncogenic driver in approximately 0.5 percent of patients with other advanced solid tumors. By targeting ROS1, taletrectinib is designed to deliver cancer-fighting therapeutics selectively to tumor cells, while sparing normal cells.

“Taletrectinib dosing of the first patient in our global Phase 2 ROS1 fusion-positive TRUST-II lung cancer trial represents a key milestone for our lead ROS1-directed clinical program,” said Bing Yan, MD, Co-Founder and Chief Medical Officer of AnHeart Therapeutics. “Based on the broad expression of ROS1 fusions across different cancer types, and our recent clinical data presented at ASCO and CSCO showing taletrectinib antitumor activity with a promising safety and efficacy profile, we are proud of advancing this investigational candidate as a potential new therapy for ROS1 fusion-positive lung cancer.”

The global Phase 2 study (TRUST-II) is a multicenter, single-arm, open label study of taletrectinib in patients of NSCLC harboring with ROS1 fusion gene. A total of 119 patients will be enrolled and divided into four cohorts, depending on past history of ROS1 tyrosine kinase inhibitor treatment. Taletrectinib will be administered 600 mg once-daily in 21-day cycles. The primary endpoint of the study is confirmed overall response rate (ORR). For additional information about the clinical trial (NCT04919811), visit www.clinicaltrials.gov.

About Taletrectinib

Taletrectinib is an investigational next-generation tyrosine kinase inhibitor (TKI) designed to effectively target ROS1 and NTRK fusion mutations with potential to treat TKI-naive or pre-treated patients. ROS1 rearrangement is estimated to be an oncogenic driver in approximately 2 to 3 percent of patients with advanced NSCLC, and NTRK rearrangement is estimated to be an oncogenic driver in approximately 0.5 percent of patients with other advanced solid tumors. More information about the ongoing China TRUST (Taletrectinib ROS1 LUng STudy) trial, global TRUST II trial and the basket trial in NTRK fusion positive solid tumors of taletrectinib (NCT04395677, NCT04919811 and NCT04617054, respectively) at www.clinicaltrials.gov.

About AnHeart Therapeutics

AnHeart Therapeutics (“AnHeart”) is a clinical-stage global biopharmaceutical company developing a broad pipeline of novel or next-generation precision oncology therapeutics with high unmet medical need. Its lead candidate, taletrectinib, is a next-generation ROS1 and NTRK inhibitor currently in Phase 2 trials in first-line and second-line ROS1 fusion positive non-small cell lung cancer (NSCLC) and NTRK fusion positive solid tumors. The Company’s pipeline also includes AB-218, a mIDH1 inhibitor in Phase 2 trials for lower grade glioma, cholangiocarcinoma, AML and other tumors and AB-329, an AXL inhibitor in Phase 1 studies to be used in combination with checkpoint inhibitor or chemotherapies in NSCLC, ovarian cancer or breast cancers. The Company operates from offices in the US and China. For more information, please visit www.anhearttherapeutics.com.

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