HSK42360 / Haisco - LARVOL DELTA

Phase 1 study of brain-penetrant BRAF inhibitor HSK42360 in adult patients with BRAF V600-mutated advanced solid tumors or recurrent primary central nervous system tumors (SNO 2025) - P1 | "An approved BRAF V600E inhibitor combined with a MEK inhibitor, had ORRs of 33% and 50% in BRAF V600E-mutated high-grade glioma (HGG) and low-grade glioma (LGG), respectively (dabrafenib US Prescribing Information, 2025). HSK42360 demonstrated a favorable safety profile and a high ORR in patients with BRAF V600-mutant PCNST. This trial is ongoing."

Clinical • Metastases • P1 data • Brain Cancer • CNS Tumor • Glioma • High Grade Glioma • Oncology • Solid Tumor

Phase 1 study of brain-penetrant BRAF inhibitor HSK42360 in adult patients with BRAF V600-mutated advanced solid tumors or recurrent primary central nervous system tumors (WFNOS 2025) - P1 | "An approved BRAF V600E inhibitor combined with a MEK inhibitor, had ORRs of 33% and 50% in BRAF V600E-mutated high-grade glioma (HGG) and low-grade glioma (LGG), respectively (dabrafenib US Prescribing Information, 2025). HSK42360 demonstrated a favorable safety profile and a high ORR in patients with BRAF V600-mutant PCNST. This trial is ongoing."

Clinical • Metastases • P1 data • Brain Cancer • Oncology • Solid Tumor

Phase I Study of HSK42360 in Malignant Brain Tumors With BRAF V600 Mutation (clinicaltrials.gov) - P1 | N=159 | Recruiting | Sponsor: Haisco Pharmaceutical Group Co., Ltd.

New P1 trial • Brain Cancer • Pediatrics • Solid Tumor • BRAF

A phase 1, multicenter, open-label study of HSK42360, a brain-penetrant BRAF inhibitor, in patients with BRAF V600-mutated solid tumors. (ASCO 2025) - P1 | "HSK42360 monotherapy was well tolerated without unexpected safety issues. Preliminary efficacy data demonstrate favorable activity of HSK42360 in pts with BRAF V600-mutated solid tumors, including primary CNS tumors. Clinical trial information: NCT06536400."

Clinical • P1 data • Brain Cancer • CNS Tumor • Ganglioglioma • Glioma • Oncology • Solid Tumor

Phase I Study of HSK42360 in Solid Tumors With BRAF V600 Mutation (clinicaltrials.gov) - P1 | N=316 | Recruiting | Sponsor: Haisco Pharmaceutical Group Co., Ltd.

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

HSK42360: A potent, brain permeable, BRAF paradox breaker for the treatment of BRAF-driven cancers (AACR 2024) - "Further characterization showed that HSK42360 did not induce homodimer or heterodimer of CRAF with CRAF or BRAF and thereby blocked reactivation of the MAPK pathway in HCT116 cells, whereas Dabrafenib significantly induced RAF dimerization and MAPK reactivation. Surprisingly, HSK42360 demonstrated promising antitumor effects in the first gen-resistant NRASmA375(NRASQ61K, BRAFV600E) CDX model, supporting its use as a follow-on therapy for current BRAFi resistance. Collectively, these preclinical studies validated that HSK42360 is a novel brain-permeable BRAF paradox breaker that exhibits outstanding antitumor activity in brain metastasis and RAF dimer-driven resistance."

Brain Cancer • Breast Cancer • CNS Tumor • Colon Cancer • Colorectal Cancer • Gastrointestinal Cancer • Glioma • Hairy Cell Leukemia • Hematological Malignancies • Leukemia • Lung Cancer • Melanoma • Non Small Cell Lung Cancer • Oncology • Ovarian Cancer • Ovarian Serous Adenocarcinoma • Solid Tumor • Thyroid Gland Carcinoma • BRAF