HH2710 / HaiHe Biopharma - LARVOL DELTA

Discovery and Characterization of HH100937, a potent and selective SOS1 inhibitor demonstrates synergistic efficacy in combination with KRAS/MAPK therapies (AACR 2024) - "HH100937 exhibited lower IC50s than BI-3406 and MTRX0902 in blocking ERK phosphorylation and cancer cell proliferation, leading to better anti-tumor efficacies in xenografts than reference compounds at same doses. HH100937 also showed synergistic effect with AMG510 in cancer cells with KRAS G12C mutation but refractory to AMG510...Our SOS1 inhibitor also exhibited synergistic effect with HH2710, a clinical-stage ERK inhibitor, in a broad panel of cancer cells with KRAS mutations.The pharmacological potency of HH100937 was highly selective over SOS2, other kinases tested or other targets in a safety panel of 47 targets...HH100937 also showed favorable DMPK properties in mice, rats and dogs, and acceptable safety profiles in vitro.Taken together, HH100937 is a highly potent and selective SOS1 inhibitor with better anti-tumor activities than some SOS1 inhibitors at clinical stage. It can be developed as mono therapy or in combination with other KRAS/MAPK targeting therapies."

Clinical • Combination therapy • Late-breaking abstract • Oncology • KRAS

A Study to Evaluate the Safety, Tolerability and Pharmacokinetics of HH2710 in Patient With Advanced Tumors (clinicaltrials.gov) - P1/2 | N=37 | Terminated | Sponsor: Haihe Biopharma Co., Ltd. | N=150 ➔ 37 | Trial completion date: Dec 2024 ➔ Mar 2023 | Recruiting ➔ Terminated | Trial primary completion date: Dec 2023 ➔ Mar 2023; Sponsor business decision

Enrollment change • Metastases • Trial completion date • Trial primary completion date • Trial termination • Lung Cancer • Melanoma • Non Small Cell Lung Cancer • Oncology • Rare Diseases • Solid Tumor • BRAF • NRAS

A Study to Evaluate the Safety, Tolerability and Pharmacokinetics of HH2710 in Patient With Advanced Tumors (clinicaltrials.gov) - P1/2 | N=150 | Recruiting | Sponsor: Haihe Biopharma Co., Ltd. | Trial completion date: Jul 2022 ➔ Dec 2024 | Trial primary completion date: Jun 2021 ➔ Dec 2023

Trial completion date • Trial primary completion date • Lung Cancer • Melanoma • Non Small Cell Lung Cancer • Oncology • Rare Diseases • Solid Tumor

A Study to Evaluate the Safety, Tolerability and Pharmacokinetics of HH2710 in Patient With Advanced Tumors (clinicaltrials.gov) - P1/2; N=150; Recruiting; Sponsor: ShangHai HaiHe Pharmaceutical; Trial completion date: Mar 2022 ➔ Jul 2022; Trial primary completion date: Dec 2020 ➔ Jun 2021

Clinical • Trial completion date • Trial primary completion date • Lung Cancer • Melanoma • Non Small Cell Lung Cancer • Oncology • Solid Tumor

[VIRTUAL] HH2710, a highly potent and selective erk1/2 inhibitor for the treatment of mapk mutant tumors (AACR-II 2020) - "In tumor xenograft models, HH2710 showed significant antitumor activity at the doses of 15, 30, and 60 mg/kg (twice per day, given orally) with the relative tumor volume at the endpoint (T/C value) of 51.0%, 18.1%, and 11.7% respectively, exhibiting improved efficacy over the front runner molecule in clinical development. Summary of pharmacokinetic parameters are listed in Table 1.The full in vitro and in vivo preclinical characterizations of HH2710 will be presented.Table 1, Pharmacokinetic parameters of HH2710 in mouse, SD rats and Beagle dogs"

Melanoma • Oncology • Solid Tumor • BRAF • MAPK1

A Study to Evaluate the Safety, Tolerability and Pharmacokinetics of HH2710 in Patient With Advanced Tumors (clinicaltrials.gov) - P1/2; N=150; Recruiting; Sponsor: ShangHai HaiHe Pharmaceutical; Not yet recruiting ➔ Recruiting; Trial primary completion date: Aug 2020 ➔ Dec 2020

Clinical • Enrollment open • Trial primary completion date

Newly added product (clinicaltrials.gov) - P2, Melanoma, NSCLC, Oncology

Pipeline update