Treeline Biosciences, Inc.

Treeline Biosciences expects to reap phase 1 data from its first three programs in 2026.\n Treeline Biosciences has surfaced from secrecy, producing a $200 million series A extension and picking three ripe programs for the clinic. The extra cash brings the Massachusetts-based oncology outfit’s total funding to $1.1 billion, while the three development programs are the first the company has disclosed.Treeline has launched phase 1 lymphoma trials for a BCL6 degrader called TLN-121 and an EZH2 inhibitor called TLN-254, according to the Sept. 3 release. The biotech has also launched clinical testing for a pan-KRAS inhibitor, TLN-372, in cancers with certain KRAS mutations. TLN-121 and TLN-372 are both internally developed by Treeline, while TLN-254 was licensed from Hengrui Pharmaceuticals in 2023 for $11 million upfront and up to $695 million in potential milestones.The biotech’s investors to date include AI Life Sciences, ARCH Venture Partners, OrbiMed, GV and KKR, among others.Treeline expects to reap phase 1 data in 2026 and plans to submit an investigational new drug (IND) application for a fourth program early next year, co-founder and CEO Josh Bilenker, M.D., wrote in a separate Sept. 3 blog post. Treeline also has three other internal programs set to enter IND-enabling studies after those phase 1 readouts, according to the post.“We aspire to create the next great enduring biopharma company,” Bilenker said in the release. “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.\"Bilenker has experience building commercial biotechs, with his prior venture Loxo Oncology developing three approved meds before being acquired by Eli Lilly for $8 billion in 2019. After the acquisition, Bilenker became Lilly’s head of cancer R&D.  At Treeline, Bilenker’s partner-in-crime is Chief Scientific Officer Jeff Engelman, M.D. Ph.D., who co-founded the company and previously served as global head of oncology at the Novartis Institutes for BioMedical Research.Treeline launched in 2021 with a series A led by Arch Venture Partners, GV and OrbiMed, but has kept a low profile since. In 2024, the tight-lipped biotech tapped 43 unnamed investors to raise nearly $422 million, the second-largest fundraising haul of the year behind only Xaira Therapeutics’ $1 billion launch.In picking its pipeline programs, Treeline focused on two key features, Bilenker wrote in his blog post. The first, ligandability, refers to the understanding of how a drug candidate binds its target, while therapeutic index represents the asset’s pharmacology, efficacy and safety.“‘Ligandability’ and ‘therapeutic index’ aren’t great elevator pitches,” Bilenker acknowledged in his post. “In a break with industry tradition, Treeline was not built around a platform or therapeutic area. We’re target pickers, assay scientists, drug engineers, computer scientists, and operations and clinical-regulatory professionals who’ve joined forces to solve hard problems together.”

After four and a half years of staying relatively quiet on its pipeline and exact financing details, Treeline Biosciences is finally coming out with some specifics on its drug candidates as a couple clinical trials are now underway . The Watertown, MA-based biotech said Wednesday it has raised another $200 million for its Series A, bringing the startup’s total funding to $1.1 billion. Former Loxo Oncology CEO Josh Bilenker has the same job title at Treeline, while ex-Novartis oncology leader Jeff Engelman is its chief scientific officer. Eli Lilly bought Loxo for $8 billion in 2019 . Treeline’s latest update makes it one of the largest total funding hauls for a Series A-stage biotech, according to an Endpoints News analysis. Only a few other biotechs have been able to raise $1 billion or more at such an early stage, including AI-driven Xaira Therapeutics . In a Wednesday blog post , Bilenker wrote that the massive funding haul will allow for the longevity of Treeline’s pipeline, without having to rely on repeat financing rounds in a treacherous capital environment that has constrained many of its peers. “If we were financed milestone to milestone, the most common model for our industry, two things were likely to happen,” Bilenker wrote. “One, we’d make choices — both technical and strategic — to always make it to the next milestone. And two, we’d focus primarily on our lead program. “Instead, we asked them to help us build a team capable of repeated invention and to resource multiple programs with complementary time horizons, technical risks and patient populations,” he added. Until this point, Treeline had stayed quiet on how much it had raised. A trickling of SEC filings had come in over the years, but never painted a full picture of the hefty capital at its disposal. “We aspire to create the next great enduring biopharma company,” Bilenker said in a separate press release. “Our funding mandate has allowed us to recruit proven scientists, rigorously test assumptions and curate a pipeline from parallel discovery efforts.” The company declined to make executives available for an interview. With the Series A, Treeline is advancing three cancer drugs into Phase 1 trials, and they’ll have data next year, Bilenker wrote in the blog. That includes two internally discovered drugs: a BCL6 degrader called TLN-121 for lymphoma, and a pan-KRAS inhibitor dubbed TLN-372 for certain KRAS mutations. Another startup, called Shenandoah Therapeutics , raised $21 million last month for its BCL6-targeting candidate. That biotech aims to convert the protein from a driver of lymphoma cell survival to one that promotes cell death. Treeline’s pipeline also includes a Phase 1-stage EZH2 inhibitor codenamed TLN-254. It in-licensed the asset from Hengrui in a $700 million deal in 2023. Hengrui has one of the most prolific R&D engines in the industry and is the go-to Chinese drugmaker for multiple Western biopharma companies, including Merck and GSK . Beyond cancer, Treeline said it is also working on neurological and autoimmune diseases. It’s developing small molecules, degraders, glues and antibody-drug conjugates. The company has already killed preclinical programs, Bilenker wrote in his blog. Treeline’s financial backers include Access Industries affiliate AI Life Sciences, ARCH Venture Partners, OrbiMed, GV, KKR and a host of crossover-type investors, like T. Rowe Price and Fidelity.

Treeline Biosciences has begun first-in-human trials for three experimental cancer therapies, while also raising an additional $200 million in a series A extension, bringing total financing to $1.1 billion since its inception over four years ago.The privately held company was co-founded by CEO Josh Bilenker, who led Loxo Oncology to its $8-billion buyout by Eli Lilly in 2019, and Chief Scientific Officer Jeff Engelman, former global head of oncology at the Novartis Institutes for BioMedical Research.The trials include two internally developed drugs – TLN-121 and TLN-372 – as well as one in-licensed asset. TLN-121 is a BCL6 degrader designed to disable a protein that lymphoma cells use to survive that is in a Phase I study enrolling patients with B-cell and T-cell lymphomas; TLN-372 is a small molecule inhibitor aimed at blocking multiple forms of KRAS for solid tumours; and TLN-254 (SHR-2554), in-licensed from Jiangsu Hengrui Pharmaceuticals after it had already undergone Phase II testing in refractory lymphoma, is an inhibitor of EZH2, a gene regulator overexpressed or mutated in certain lymphomas. The latter is recruiting patients in a Phase I trial for peripheral and cutaneous T-cell lymphomas.Bilenker said Treeline's approach has been made possible by its unusually large funding base that "has carried us for the last 4.5 years and will continue to do so for many more." He noted that the company has been able to advance multiple programmes in parallel while discontinuing others that didn't meet internal benchmarks. "Having the luxury of moving on from programmes is probably the greatest gift our funding mandate has given us," he said.Treeline launched in 2021 with $200 million in initial funding, followed by a KKR-led expansion in 2022 that brought the company to over 130 employees and a $421.8-million round last October. Investors in the series A extension include AI Life Sciences, ARCH Venture Partners, OrbiMed, GV and KKR among others.According to Bilenker, Treeline's discovery engine, which integrates computational tools with lab-based biology, emphasises ligandability and therapeutic index. "Our pipeline includes programmes that are, to our knowledge, the first to establish ligandability. We have other programmes that were structurally enabled from the outset. Unsurprisingly, the latter category gets to the clinic first, as is the case with our first INDs," he said."Whatever the organising story, all biotech and pharma companies are eventually measured the same way – on their clinical data," Bilenker added.