On October 13, 2021 Turning Point Therapeutics, Inc. (NASDAQ: TPTX), a precision oncology company developing next-generation therapies that target genetic drivers of cancer, and EQRx, a new type of pharmaceutical company committed to developing and delivering important new medicines to patients at radically lower prices, reported a clinical collaboration to evaluate elzovantinib (TPX-0022), Turning Point’s drug candidate targeting MET, SRC, and CSF1R, in combination with aumolertinib, EQRx’s drug candidate targeting EGFR, in patients with EGFR mutant MET-amplified advanced non-small cell lung cancer (NSCLC) (Press release, Turning Point Therapeutics, OCT 13, 2021, View Source [SID1234591242]).

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Under the terms of the agreement, Turning Point will sponsor and conduct a Phase 1b/2 clinical trial to evaluate the safety, tolerability and preliminary efficacy of the combination regimen and will assume all costs associated with the trial. EQRx will provide aumolertinib at no cost. Turning Point is targeting initiation of the clinical trial in 2022, pending filing of an investigational new drug (IND) application by the U.S. Food and Drug Administration (FDA).

Preclinical data suggest the combination of MET and EGFR inhibition has the potential to increase anti-tumor activity based on complementary mechanisms. It is estimated that 15 to 20% of patients who progress on a first-line EGFR inhibitor develop MET amplification as the basis of acquired resistance.

"We believe the combination of elzovantinib with aumolertinib could provide an important potential treatment option for patients who develop MET amplification as acquired resistance to an EGFR inhibitor, where no approved therapies are available today," said Athena Countouriotis, M.D., president and chief executive officer of Turning Point. "We are pleased to have EQRx as our collaboration partner and look forward to initiating our Phase 1b/2 SHIELD-2 study of the combination."

"This collaboration marks the launch of the EQRx-Inside Platform, a unique development-to-commercialization platform designed to accelerate access to potentially life-enhancing combination therapies and create efficiencies for partners, physicians, and health systems," said Melanie Nallicheri, chief executive officer of EQRx. "We are pleased to partner with Turning Point and believe this collaboration will be the first of many that will broaden patient access to important combination clinical trials and innovative potential cancer therapies such as aumolertinib and elzovantinib."

About Elzovantinib
Elzovantinib is a multi-targeted orally bioavailable Type I TKI with a novel macrocyclic structure that potently inhibits MET, SRC and CSF1R, in preclinical assays. MET alterations, including point mutations, amplifications, fusions, exon 14 skipping, and the generation of HGF-MET autocrine loops have been reported in many cancers. SRC inhibition may have the potential to reduce or abolish certain oncogenic signaling, and the targeting of CSF1R leads to the modulation of tumor associated macrophages.

Preliminary clinical data from the ongoing Phase 1 SHIELD-1 study of single-agent elzovantinib presented at the 2021 AACR (Free AACR Whitepaper)-NCI-EORTC Conference in October 2021, demonstrated preliminary clinical activity, including objective responses across multiple tumor types and a generally tolerable safety profile. The U.S. Food and Drug Administration has granted elzovantinib Orphan Drug designation for the treatment of gastric cancer, including gastroesophageal junction cancer, and Fast Track designation for the treatment of patients with MET-amplified advanced or metastatic gastric cancer or gastroesophageal junction (GEJ) adenocarcinoma after prior chemotherapy.

About Aumolertinib
Aumolertinib 110 mg once-daily is a prescription medicine approved in China as AMEILE for the treatment of patients with metastatic EGFR T790M mutation-positive NSCLC, as detected by a genomic test, who have progressed on or after prior EGFR TKI therapy. Aumolertinib is a novel, irreversible EGFR-TKI that selectively inhibits both EGFR sensitizing and resistance mutations with high selectivity over wild-type EGFR. Aumolertinib was approved in China in March 2020 based on the large single arm Phase 2 APOLLO study in second-line settings. The ongoing Phase 3 AENEAS trial in first-line settings met its primary endpoint of progression-free survival and topline results were presented at the 2021 ASCO (Free ASCO Whitepaper) Annual Meeting.

Hansoh Pharma and EQRx have partnered to expand global access to aumolertinib. EQRx holds the development and commercialization rights to aumolertinib outside of Greater China and is pursuing regulatory discussions in multiple countries.