- ALTA3263 is a potential best-in-class KRAS-selective small molecule inhibitor that potently targets >90% of KRAS mutations
- ALTA3263 is designed for complete KRAS target coverage, which will be required to achieve breakthrough efficacy and safety for patients with KRAS-driven cancers
SAN DIEGO--(BUSINESS WIRE)--Alterome Therapeutics, Inc., a clinical-stage biopharmaceutical company pioneering the development of next-generation, small molecule targeted therapies for the treatment of cancer, today announced that the first patient has been dosed in the Phase 1/1b trial of ALTA3263 in adults with KRAS mutant solid tumors.
ALTA3263 is an oral KRAS-selective inhibitor specifically designed to potently inhibit the KRAS “ON” (active) state of greater than 90% of all KRAS mutations and to provide complete target coverage in tumors. These properties have the potential to translate into best-in-class safety and efficacy. KRAS driver mutations are found in greater than 20% of all patients with metastatic cancer, with the majority in non-small cell lung cancer (NSCLC), pancreatic ductal carcinoma (PDAC), and colorectal cancer (CRC).
“With this trial, we hope to bring a breakthrough therapy to the many patients with KRAS-driven cancers who are still underserved,” said Andrew Chi, M.D., Ph.D., Chief Medical Officer of Alterome. “We have shown in preclinical studies that ALTA3263 has the attributes to potentially address this significant unmet need and transform patient outcomes.”
“While progress has been made in KRAS mutant cancers, we still regularly see patients who have exhausted all available effective treatment options and also suffer from toxic side effects of current therapies,” said Anthony Tolcher, M.D., FRCPC, Founder of NEXT Oncology and primary investigator on the ALTA3263 Phase 1/1b trial. “We are excited to participate in this trial, and hope that ALTA3263 will usher in the next generation of KRAS targeted therapies that promise greater efficacy and improved tolerability and safety for patients.”
The Phase 1/1b, open-label, dose-escalation and multiple cohort study is evaluating the safety, tolerability, pharmacokinetics, and preliminary clinical activity of ALTA3263 in adults with advanced unresectable or metastatic solid tumors with KRAS mutations (NCT06835569).
About ALTA3263
ALTA3263 is a non-covalent, orally bioavailable, highly potent KRAS isoform-selective dual ON/OFF state inhibitor designed to target >90% of all KRAS driver mutations in cancer. While mutation-specific KRAS inhibitors that target the KRAS OFF-state have demonstrated clinical benefit, highly prevalent KRAS mutations such as G12D and G12V exist predominantly in the ON-state and remain a substantial unmet medical need. ALTA3263 inhibits KRAS with picomolar to low single-digit nanomolar potency and targets both the ON and OFF states while exhibiting high selectivity for KRAS over HRAS and NRAS to allow for a favorable therapeutic index. These properties, together with excellent pharmacokinetic and tolerability profiles enable complete and continuous target coverage to inhibit KRAS-driven cancers. ALTA3263 led to deep regressions in multiple KRAS mutant preclinical models while being well-tolerated during prolonged oral dosing. These data were presented in an oral presentation at the 2024 EORTC-NCI-AACR (ENA) Symposium. For more information on ALTA3263, visit https://www.alterome.com/programs/.
About Alterome Therapeutics, Inc.
Alterome Therapeutics, Inc. is a clinical-stage precision oncology biotechnology company developing alteration-specific therapeutics to address high-value and validated oncogenic drivers. Our pipeline includes two Phase 1 therapies in development for solid tumors: ALTA2618, a first-in-class, oral mutation-selective inhibitor for AKT1 E17K-driven cancers, and ALTA3263, a potential best-in-class, KRAS-selective (ON/OFF) inhibitor for KRAS-driven cancers. Alterome has raised more than $231 million in venture capital to date and is led by a team of precision oncology R&D leaders with a history of developing marketed oncology small molecule drugs.
For more information, visit www.alterome.com and follow us on LinkedIn and Bluesky.
Contacts
Investors:
Scott Moorefield
Alterome Therapeutics
investors@alterome.com
Media:
Michael Galfetti
Ten Bridge Communications
alterome@tenbridgecommunications.com
