Alpelisib

Laekna (HKEX: 02105) has licensed its pre-clinical PI3Kα inhibitor LAE118 to US-based Vasque Bio in a deal worth up to USD 527 million. Vasque will serve as a rare-disease-focused channel for the global development of Laekna’s next-generation mutant-selective kinase inhibitor, which has cleared IND review in both the US and China. The LAE118 license agreement, announced on June 9, 2026, grants Vasque Bio exclusive worldwide rights excluding Greater China to develop, manufacture, and commercialize the compound. The deal’s equity component — Laekna’s right to acquire up to a high-teen percentage of Vasque Bio stock at no additional cost — gives the originator direct exposure to any future exit. Under the terms, Laekna receives a USD 10 million non-refundable upfront payment, up to USD 517 million in combined development and sales milestones, and tiered royalties ranging from single-digit to double-digit percentages on any future net sales. A further clause entitles Laekna to up to 50% of the value of any qualifying strategic transaction — such as an acquisition or sublicense — that Vasque Bio enters involving LAE118. That provision is structurally uncommon and suggests Laekna negotiated aggressively to guard against a scenario where Vasque Bio exits cheaply before milestones are earned. Laekna’s PI3Kα inhibitor LAE118 is described by Laekna as a novel PI3Kα pan-mutant selective inhibitor, designed to target the mutant forms of the PI3Kα enzyme while sparing the wild-type protein. First-generation PI3Kα inhibitors, including Novartis’s alpelisib (Piqray/Vijoice), inhibit both mutant and wild-type enzyme, producing on-target toxicities — particularly hyperglycemia — that limit dosing and combination potential. Mutant-selective agents aim to widen the therapeutic window by concentrating activity on disease-driving variants. According to Laekna, LAE118 is being actively developed into clinical studies for PIK3CA-mutant solid tumors in both China and the US. The partnership introduces an unusual indication split. Laekna describes its own development focus as oncology, while Vasque Bio — backed by The Column Group and F-Prime — is described as a company dedicated to rare diseases. PIK3CA gain-of-function mutations drive not only common cancers but also a spectrum of rare overgrowth conditions known as PIK3CA-related overgrowth spectrum disorders, where targeted PI3Kα inhibition has shown biological rationale. Industry and transaction context The LAE118 license agreement arrives in the middle of a concentrated wave of large-pharma and venture capital activity targeting next-generation PI3Kα mutant-selective inhibitors. In March 2026, Novartis agreed to acquire Synnovation Therapeutics’ pan-mutant selective PI3Kα program SNV4818 for up to USD 3 billion, paying USD 2 billion upfront — a transaction that set a high-water mark for the class. The competitive field for pan-mutant selective PI3Kα inhibitors has become notably crowded. Relay Therapeutics’ zovegalisib (RLY-2608), an allosteric pan-mutant isoform-selective inhibitor, is in a Phase III pivotal study in HR+/HER2- breast cancer. Eli Lilly’s tersolisib (STX-478), acquired via Scorpion Therapeutics, has entered a front-line pivotal trial. Celcuity’s gedatolisib, a pan-PI3K/mTOR inhibitor, met the primary endpoint of the Phase III VIKTORIA-1 trial against alpelisib in PIK3CA-mutant breast cancer. LAE118 enters this landscape without clinical efficacy data and with multiple competitors already generating late-stage readouts. The structural features of the Laekna Vasque Bio partnership are worth examining in the context of how Chinese biotech companies have been structuring ex-China deals. The 50% strategic transaction participation right — entitling Laekna to half the value of any qualifying M\&A or sublicense involving LAE118 — goes beyond standard royalty and milestone protections. It functions more like a co-ownership clause than a typical licensor protection, and reflects a pattern seen in other recent China-to-Western deals where originators have sought to retain economic exposure beyond conventional milestone structures. This article was generated with AI assistance and reviewed and edited by the AllSci editorial team Explore more at AllSci News: https://allsci.com/news/ Leave a Reply Cancel reply Your email address will not be published. Required fields are marked * Comment * Name * Email * Website Privacy Terms About Us Copyright © 2026. AllSci Corp. All rights reserved.

Two regimens containing Celcuity's multi-target PAM inhibitor gedatolisib halved the risk of disease progression or death versus Novartis' PI3Kα inhibitor Piqray (alpelisib) in adults with hormone receptor (HR)-positive, HER2-negative, PIK3CA mutated, locally advanced or metastatic breast cancer. The statistically significant and clinically meaningful findings come from the Phase III VIKTORIA-1 trial, which were presented Tuesday at the American Society of Clinical Oncology (ASCO) annual meeting. “By comprehensively blocking the PI3K/AKT/mTOR, or PAM, pathway, gedatolisib…showed it can offer these patients two times the likelihood of survival without disease progression or death relative to a single-target inhibitor of the PAM pathway," said co-principal investigator Sara Hurvitz. "With these results, the gedatolisib regimens, if approved, represent a new potential standard of care for patients with HR+, HER2-negative, PIK3CA mutant advanced breast cancer whose disease progressed on or after treatment with a CDK4/6 inhibitor.” VIKTORIA-1 already produced positive results in the PIK3CA wild-type cohort, with a progression-free survival (PFS) benefit of 76% for gedatolisib compared to fulvestrant — the FDA is set to decide on approval in this patient population by July 17. And last month, Celcuity said that the study, which enrolled participants who progresed on, or after, treatment with a CDK4/6 inhibitor and an aromatase inhibitor, also hit its primary endpoint against Piqray in the PIK3CA-mutant cohort. Results presented at ASCO showed that a triplet regimen of gedatolisib, fulvestrant and Pfizer's CDK4/6 inhibitor Ibrance (palbociclib) reduced the risk of disease progression or death by 50% versus Piqray plus fulvestrant. Median PFS in the two arms was 11.1 months and 5.6 months, respectively. Meanwhile, the dual regimen of gedatolisib plus fulvestrant reduced the risk of disease progression or death by 49% compared to Piqray plus fulvestrant, with median PFS of 11.3 months. Celcuity added that the gedatolisib triplet regimen demonstrated an objective response rate of 48.9%, which it was 35.7% for the dual regimen, compared to 26% for Piqray plus fulvestrant. Further, the median duration of response was 15.7 months for the gedatolisib triplet regimen, versus 24.2 months for the doublet regimen and 7.5 months for Piqray plus fulvestrant. “Both gedatolisib regimens were well-tolerated with very few VIKTORIA-1 patients discontinuing treatment due to an adverse event," said Igor Gorbatchevsky, Celcuity's chief medical officer. Treatment-related adverse events that led to the discontinuation of study treatment occurred in 2.6% of patients in the gedatolisib-triplet group, 3.8% in the gedatolisib doublet group, and 7.1% in the Piqray plus fulvestrant group. While there was one grade 5 TRAE in the gedatolisib-triplet group, the company noted that this was related to Ibrance — there were no similar events in the gedatolisib-doublet group, versus two in the Piqray plus fulvestrant arm. The content above comes from the network. if any infringement, please contact us to modify.