APS03118 / Applied Pharmaceutical Sci - LARVOL DELTA

Discovery of APS03118, a Potent and Selective Next-Generation RET Inhibitor with a Novel Kinase Hinge Scaffold. (PubMed, J Med Chem) - P1 | "Optimized pharmacokinetic properties (38.9% oral bioavailability in monkey) and central nervous system penetration support clinical translation. APS03118 is currently in phase Ib trials (NCT05653869) for patients progress on first-generation SRIs, offering a promising strategy to address acquired resistance."

Journal • Oncology • CCDC6 • FLT3 • KIF5B

Development of a novel next-generation RET inhibitor (AACR 2024) - "Two first-generation selective RET inhibitors selpercatinib and pralsetinib have been approved for patients with RET-driven solid tumors including non-small cell lung cancer (NSCLC) and thyroid cancer. Taken together, APS03118 is a novel highly potent and selective next-generation RET inhibitor overcoming resistance following treatment with the first-generation RET inhibitors. APS03118 warrants further clinical development."

Brain Cancer • Endocrine Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • Thyroid Gland Carcinoma • RET

A Study of APS03118 in Advanced Solid Tumors Harboring RET Mutations or Fusions (clinicaltrials.gov) - P1 | N=35 | Recruiting | Sponsor: Applied Pharmaceutical Science, Inc.

Metastases • New P1 trial • Oncology • Solid Tumor • RET

The development of APS03118, a potent next-generation RET inhibitor for treating RET-inhibitor-resistant patients. (ASCO 2022) - "Selective RET inhibitors selpercatinib and pralsetinib were recently approved by the FDA and EMA for patients with RET-dependent NSCLC and thyroid cancers. APS03118 is a novel highly selective next-generation RET inhibitor that possesses potent in vitro and in vivo activity against a diverse range of RET alterations, including SFMs-mediated resistance. APS03118 has received IND approval and Fast Track Designation from FDA, and a first-in-human phase 1 trial for patients with RET-driven solid tumors with activating RET alterations is planned for 2022."

Clinical • Endocrine Cancer • Immunology • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • Thyroid Gland Carcinoma • CCDC6 • KDR • KIF5B • RET

The preclinical selectivity and activity of APS03118, a highly selective and potent next-generation RET inhibitor (AACR 2022) - "Selective RET inhibitors selpercatinib and pralsetinib were recently approved by the FDA and EMA for patients with RET-dependent NSCLC and thyroid cancers. APS03118 is a novel highly selective next-generation RET inhibitor that possesses potent in vitro and in vivo activity against a diverse range of RET alterations, including SFMs-mediated resistance. A first-in-human phase 1 trial for patients with RET-driven solid tumors with activating RET alterations is planned for 2022."

Preclinical • Endocrine Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • Thyroid Gland Carcinoma • CCDC6 • KDR • KIF5B • RET

Applied Pharmaceutical Science Inc. Announces FDA Approval of Investigational New Drug Application for APS03118, a Next generation RET Original New Drug for Unlimited Cancers (PRNewswire) - "Applied Pharmaceutical Science...has recently announced the Investigational New Drug (IND) application for its self-developed breakthrough new drug APS03118, a next generation selective RET inhibitor, has been approved by the U.S. Food and Drug Administration (FDA). The clinical application is also in the process of being submitted to the National Medical Products Administration (NMPA) in China, and a global multi-center clinical trial is in the pipeline for initiation in the second quarter of 2022 in the U.S., China and Australia etc."

IND • Non-US regulatory • Breast Cancer • Colorectal Cancer • Gastrointestinal Cancer • Genito-urinary Cancer • Gynecologic Cancers • Head and Neck Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Ovarian Cancer • Pancreatic Cancer • Solid Tumor • Thyroid Gland Carcinoma