Treeline Biosciences announced the initiation of Phase 1 clinical trials for three oncology programs while securing $200 million in additional funding, marking a significant milestone for the clinical-stage biotechnology company. The trials evaluate TLN-121, a BCL6 protein degrader for lymphomas; TLN-372, a pan-KRAS inhibitor for solid tumors; and TLN-254, an EZH2 inhibitor for lymphomas.
The funding round brings Treeline's total capital raised to $1.1 billion, with investors including AI Life Sciences, ARCH Venture Partners, OrbiMed, GV, KKR, and accounts advised by T. Rowe Price Associates, among others.
Novel Approaches to Challenging Targets
BCL6 Degradation Strategy
TLN-121 targets BCL6, a naturally occurring protein that lymphoma cells exploit to silence genes that would otherwise block their growth and survival. The protein degrader is designed to remove BCL6 from cancer cells while avoiding off-target effects that could cause toxicity, potentially enabling combination use with standard-of-care lymphoma therapies. The Phase 1 trial (NCT07082803) is enrolling patients with B-cell and T-cell lymphomas.
Pan-KRAS Inhibition
TLN-372 addresses a significant therapeutic gap in oncology, as approximately one in four adult cancers harbor a KRAS alteration. While FDA-approved medicines exist for G12C mutations, other KRAS variants remain unaddressed by targeted therapies. TLN-372 is a small molecule inhibitor with novel chemistry designed for deep, continuous pan-KRAS inhibition and possesses favorable drug-like properties. The Phase 1 trial will enroll patients with KRAS-altered solid tumors.
EZH2 Inhibition Program
TLN-254, an in-licensed program, targets EZH2, which regulates gene expression and is often overexpressed or mutated in cancers. The small molecule inhibitor was acquired after Phase 2 testing in refractory lymphoma. The Phase 1 trial (NCT06733441) is enrolling patients with peripheral and cutaneous T-cell lymphomas.
Leadership and Strategic Vision
"We aspire to create the next great enduring biopharma company," said Josh Bilenker, M.D., Treeline's Co-Founder and CEO. "Our funding mandate has allowed us to recruit proven scientists, rigorously test assumptions and curate a pipeline from parallel discovery efforts. BCL6 and KRAS are formidable targets that required difficult chemistry and novel assay development. We hope these programs deliver for patients and create momentum for our next set of clinical entries."
The company is co-founded by Bilenker and Jeff Engelman, M.D., Ph.D., both oncologists with extensive R&D leadership experience. Bilenker previously founded Loxo Oncology, which developed three FDA-approved medicines, while Engelman served as director of thoracic oncology at Massachusetts General Hospital and later as global head of oncology at the Novartis Institutes for BioMedical Research.
Technology Platform and Pipeline
Treeline's internal R&D team utilizes leading-edge computational tools to prioritize workflow and accelerate timelines. The company's therapeutic focus spans cancer, neurological, and autoimmune diseases, with programs encompassing small molecules, degraders and glues, and targeted therapy ADCs (TT-ADCs). The team and pipeline were built for scaled invention and company longevity.
