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

Expert consensus on iruplinalkib for the treatment of ALK-positive non-small cell lung cancer (2026 edition) (PubMed, Zhonghua Zhong Liu Za Zhi) - "Currently, the China National Medical Products Administration (NMPA) has approved ten ALK-TKIs, including crizotinib, ceritinib, alectinib, ensartinib, brigatinib, lorlatinib, iruplinalkib, envonalkib, dirozalkib and conteltinib. This consensus provides systematic and comprehensive update of clinical research data on iruplinalkib published before June 25, 2026, based on the 2024 edition. It covers common clinical issues and provides corresponding recommendations for the use of iruplinalkib in the treatment of ALK-positive NSCLC."

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

Shouyao Holdings (Beijing) Co., Ltd…announced it has received marketing approval from the National Medical Products Administration (NMPA) for its CT-707, a second-generation ALK inhibitor. (flcube.com) - "The approval allows CT-707 to be used in patients with ALK-positive locally advanced or metastatic non-small cell lung cancer (NSCLC) who have not previously received treatment with an anaplastic lymphoma kinase (ALK) inhibitor."

China approval • Non Small Cell Lung Cancer

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

Acquired EGFR L858R mutation following ALK-TKI resistance in lung adenocarcinoma: a case report. (PubMed, Front Oncol) - "We present a patient with Anaplastic lymphoma kinase (ALK) fusion lung adenocarcinoma who received sequential treatment with ALK tyrosine kinase inhibitor (TKI) (crizotinib, PFS:32.3 months and then conteltinib, PFS: 29 months). Subsequently, the patient switched to third generation EGFR-TKI treatment with almonertinib. This case suggests EGFR mutation is one of the mechanisms of ALK-TKI resistance, highlights the value of re-biopsy in identifying potentially targetable resistance mechanisms and underscores the spatiotemporal heterogeneity of tumors under the selective pressure of ALK-TKI."

Journal • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • ALK • EGFR

Pathway -targeted combination screening in 3D -spheroids reveals synergistic interactions with everolimus in pancreatic neuroendocrine tumors (ENETS 2026) - " The AKT inhibitor Tuvusertib showed the strongest mo - notherapy effect, although its synergy combined with everolimus was limited. Cytostatic synergy with everolimus was observed with JAK/STAT pathway inhibitors (Conteltinib, Pacritinib) in BON spheroids and with ERK1/2 and PI3K α inhibitors (ASTX029, Gil - melisib) in BON-R spheroids...Cytoto - xic synergy with everolimus was mainly associated with inhibition of the MAPK/ERK pathway, involving ERK inhibitors (Tizaterkib, Ulexertinib) in BON-R spheroids and MEK inhibitors (Binimetinib, Cobimetinib, Trametinib) in both models. High-content 3D spheroid screening integrating NOGR-based growth metrics identified multiple synergistic inter - actions between everolimus and inhibitors targeting interconnec - ted signaling cascades. These findings highlight the potential of rational pathway-targeted combinations to overcome resistance and enhance therapeutic efficacy in pNET, warranting further preclinical investigation to..."

Gastrointestinal Neuroendocrine Tumor • Neuroendocrine Tumor • Oncology • Solid Tumor • PIK3CA

Study of SY-5933 Plus CT-707 in Advanced Solid Tumors With KRAS p.G12C Mutation (clinicaltrials.gov) - P1/2 | N=102 | Not yet recruiting | Sponsor: Shouyao Holdings (Beijing) Co. LTD

New P1/2 trial • Colorectal Cancer • Lung Cancer • Non Small Cell Lung Cancer • Solid Tumor • KRAS

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

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