conteltinib (SY-707) / Centaurus Biopharma, Shouyao Holdings - LARVOL DELTA

Deep Learning-Based Drug Compounds Discovery for Gynecomastia. (PubMed, Biomedicines) - "DTI analysis and DeepPurpose predictions identified 12 potential drugs, including conteltinib, yifenidone and vosilasarm, with high predicted binding affinities to the target genes. The findings highlight the effectiveness of combining text mining and artificial intelligence in drug discovery. This innovative method provides a new avenue for developing specific treatments for gynecomastia and underscores the need for further experimental validation and optimization of prediction models to support novel drug development."

Journal • IGF1 • TGFB1

Targeting FAK to improve the therapy of KRAS G12C mutant cancers (AACR 2024) - "In conclusion, our results demonstrate that CT-707 has the potential to enhance the efficacy of SY-5933 by suppressing adaptive FAK activation under KRAS G12C inhibition. This provides a rationale for an innovative combination therapy to improve outcomes in patients with KRAS G12C mutated cancers."

Colorectal Cancer • Gastrointestinal Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Pancreatic Cancer • Solid Tumor • KRAS

Roles and inhibitors of FAK in cancer: current advances and future directions. (PubMed, Front Pharmacol) - "To date, numerous FAK inhibitors, including IN10018, defactinib, GSK2256098, conteltinib, and APG-2449, have been developed, which have demonstrated positive anti-tumor effects in preclinical studies and are undergoing clinical trials for several types of tumors. This review aims to clarify FAK's role in cancer, offering a comprehensive overview of the current status and future prospects of FAK-targeted therapy and combination approaches. The goal is to provide valuable insights for advancing anti-cancer treatment strategies."

Journal • Review • Oncology

Conteltinib (CT-707) in patients with advanced ALK-positive non-small cell lung cancer: a multicenter, open-label, first-in-human phase 1 study. (PubMed, BMC Med) - P1 | "In this study, conteltinib showed manageable safety profile, favorable PK properties, and anti-tumor activity in advanced ALK-positive NSCLC patients. The recommended phase 2 dose was determined to be 600 mg QD for ALK TKI-naïve patients and 300 mg bis in die (BID) for patients who received crizotinib previously."

Journal • P1 data • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • ALK

Safety, Pharmacokinetics and Efficacy of CT-707, Toripalimab and Gemcitabine in Advanced Pancreatic Cancer (clinicaltrials.gov) - P1/2 | N=114 | Recruiting | Sponsor: Shouyao Holdings (Beijing) Co. LTD

Combination therapy • New P1/2 trial • Gastrointestinal Cancer • Hepatology • Oncology • Pancreatic Adenocarcinoma • Pancreatic Cancer • Solid Tumor

CT-707 overcomes hypoxia-mediated sorafenib resistance in Hepatocellular carcinoma by inhibiting YAP signaling. (PubMed, BMC Cancer) - "Overall, this study not only favors the development of this novel multi-kinase inhibitor CT-707 as a therapeutic agent against HCC, but also provides a potential strategy to overcome the hypoxia-mediated resistance to sorafenib in HCC patients."

Journal • Gastrointestinal Cancer • Hepatocellular Cancer • Oncology • Solid Tumor

CT-707 Overcomes Resistance of crizotinib through activating PDPK1-AKT1 pathway by targeting FAK. (PubMed, Curr Cancer Drug Targets) - "These findings indicate that CT-707 may be a promising therapeutic agent against crizotinib-resistance in NSCLC."

Journal • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Thoracic Cancer