BGB-58067 / BeOne Medicines - LARVOL DELTA

First-in-human trial of BGB-58067, an MTA-Cooperative PRMT5 Inhibitor, in MTAP-deficient advanced tumors (ESMO 2026) - No abstract available

First-in-human • Metastases • P1 data • Oncology • MTAP

A Study to Investigate the Relative Bioavailability of 2 Tablet Formulations and the Effect of Food on the Pharmacokinetics of BGB-58067 in Healthy Participants (clinicaltrials.gov) - P1 | N=32 | Recruiting | Sponsor: BeOne Medicines | Not yet recruiting ➔ Recruiting

Enrollment open

BeOne Medicines and Revolution Medicines Announce Clinical Development and Regional Commercialization Collaboration (Businesswire) - "Potential drug combinations for development as part of the clinical collaboration will include certain BeOne assets and Revolution Medicines’ four clinical RAS(ON) inhibitors: daraxonrasib, a RAS(ON) multi-selective inhibitor; zoldonrasib, a RAS(ON) G12D-selective inhibitor; elironrasib, a RAS(ON) G12C-selective inhibitor; and RMC-5127, a RAS(ON) G12V-selective inhibitor. Planned combination studies include: BeOne’s MTA-cooperative PRMT5 inhibitor, BGB-58067, and an EGFR x MET x MET trispecific antibody, BG-T187, with either daraxonrasib or zoldonrasib....Under the regional rights agreement, Revolution Medicines has granted BeOne exclusive rights in select Asian markets to develop and commercialize or solely commercialize, depending on the market, these four clinical-stage RAS(ON) inhibitors."

Licensing / partnership • Solid Tumor

BGB-58067 (MTA-cooperative PRMT5 inhibitor): Received U.S. FDA Orphan Drug Designation for the treatment of adult patients with pancreatic ductal adenocarcinoma. (Businesswire)

Orphan drug • Pancreatic Ductal Adenocarcinoma

A Study to Investigate the Relative Bioavailability of 2 Tablet Formulations and the Effect of Food on the Pharmacokinetics of BGB-58067 in Healthy Participants (clinicaltrials.gov) - P1 | N=32 | Not yet recruiting | Sponsor: BeOne Medicines

New P1 trial

An Investigational Study of BGB-58067 As a Single Agent and in Combination With Anticancer Agents in Participants With Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=235 | Sponsor: BeOne Medicines | N=97 ➔ 235

Enrollment change • First-in-human • Oncology • Solid Tumor • MTAP

A Study to Investigate the Effect of the CYP3A Inducer Phenytoin and the CYP3A Inhibitor Itraconazole on the Pharmacokinetics of BGB-58067 in Healthy Participants (clinicaltrials.gov) - P1 | N=30 | Recruiting | Sponsor: BeOne Medicines | Not yet recruiting ➔ Recruiting

Enrollment open

A Study to Investigate the Effect of the CYP3A Inducer Phenytoin and the CYP3A Inhibitor Itraconazole on the Pharmacokinetics of BGB-58067 in Healthy Participants (clinicaltrials.gov) - P1 | N=30 | Not yet recruiting | Sponsor: BeOne Medicines

New P1 trial

BGB-58067 in Newly Diagnosed Glioblastoma Patients With MTAP-Deleted Tumors (clinicaltrials.gov) - P1 | N=78 | Recruiting | Sponsor: Nader Sanai | Not yet recruiting ➔ Recruiting | Trial completion date: Apr 2028 ➔ Nov 2028 | Trial primary completion date: Apr 2027 ➔ Nov 2027

Enrollment open • Trial completion date • Trial primary completion date • Brain Cancer • Glioblastoma • Oncology • Solid Tumor

An Investigational Study of BGB-58067 As a Single Agent and in Combination With Anticancer Agents in Participants With Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=525 | Recruiting | Sponsor: BeOne Medicines | N=244 ➔ 525 | Trial completion date: Jan 2029 ➔ Sep 2027 | Trial primary completion date: Jan 2029 ➔ Sep 2027

Enrollment change • First-in-human • Trial completion date • Trial primary completion date • Oncology • Solid Tumor • MTAP

An Investigational Study of BGB-58067 As a Single Agent and in Combination With Anticancer Agents in Participants With Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=244 | Recruiting | Sponsor: BeOne Medicines | N=79 ➔ 244

Enrollment change • First-in-human • Oncology • Solid Tumor • MTAP

BGB-58067, a brain-penetrative MTA-cooperative PRMT5 inhibitor, demonstrates promising anti-tumor activity and favorable selectivity in tumors with MTAP-deletion (AACR 2026) - "BGB-58067 shows favorable nonclinical safety profile in the GLP studies, as well as good selectivity in an in vitro SafetyScreen87-off target profiling study. In conclusion, BGB-58067 demonstrates robust potency and selectivity, providing a favorable safety margin for patients, with high potential for the treatment of brain tumors and brain metastases."

Brain Cancer • Oncology • Solid Tumor • MTAP

Trial in progress: A first-in-human phase 1a/b study of BGB-58067, an MTA-cooperative PRMT5 inhibitor, in patients with advanced solid tumors and MTAP deficiency (AACR 2025) - P1 | "For phase 1b, the primary objectives are to determine the recommended phase 2 dose and to assess the antitumor activity (ORR per investigator); secondary objectives are to further assess antitumor activity (DOR, DCR and progression-free survival per investigator) and safety/tolerability of BGB-58067. As of December 2024, the trial is actively recruiting patients in Australia, China, and the United States."

Clinical • First-in-human • Metastases • P1 data • Bladder Cancer • Brain Cancer • CNS Tumor • Genito-urinary Cancer • Glioblastoma • Oncology • Solid Tumor • MTAP • PRMT5

A Phase 1a/b Study Investigating the Safety, Tolerability, Pharmacokinetics, Pharmacodynamics, and Preliminary Antitumor Activity of PRMT5 Inhibitor BGB-58067 Alone and in Combination with Anticancer Agents in Patients With Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=63 | Recruiting | Sponsor: BeOne Medicines | N=44 ➔ 63

Enrollment change • First-in-human • Oncology • Solid Tumor • MTAP

Phase 0/2 PD-Trigger Study of BGB-58067 in Newly Diagnosed Glioblastoma Patients With MTAP-Deleted Tumors (clinicaltrials.gov) - P1 | N=78 | Not yet recruiting | Sponsor: Nader Sanai

New P1 trial • Brain Cancer • Glioblastoma • Oncology • Solid Tumor

An Investigational Study of BGB-58067 As a Single Agent and in Combination With Anticancer Agents in Participants With Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=244 | Recruiting | Sponsor: BeOne Medicines | Trial completion date: Jun 2027 ➔ Jan 2029 | Trial primary completion date: Jun 2027 ➔ Jan 2029

Trial completion date • Trial primary completion date • Oncology • Solid Tumor

An Investigational Study of BGB-58067 As a Single Agent and in Combination With Anticancer Agents in Participants With Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=237 | Recruiting | Sponsor: BeiGene | N=92 ➔ 237 | Trial completion date: Nov 2026 ➔ Jun 2027 | Trial primary completion date: Nov 2026 ➔ Jun 2027

Enrollment change • Trial completion date • Trial primary completion date • Oncology • Solid Tumor

BeiGene Announces Global Licensing Agreement for MAT2A Inhibitor (Businesswire) - "BeiGene...announced it has entered into a global licensing agreement with CSPC Zhongqi Pharmaceutical Technology...for SYH2039, a novel methionine adenosyltransferase 2A (MAT2A)-inhibitor being explored for solid tumors....'This MAT2A inhibitor is a valuable addition to our solid tumor pipeline, and we’re eager to explore its potential, particularly in combination with our internally developed PRMT5 inhibitor, BGB-58067'....BGB-58067, which is on track to enter the clinic before the end of the year, is designed to avoid on-target hematological toxicity seen with first-generation PRMT5 inhibitors....Under the terms of the agreement, BeiGene has an exclusive license to develop, manufacture and commercialize SYH2039 worldwide. CSPC will receive upfront and time-based payments totaling $150 million and will be eligible for payments upon the achievement of certain development and commercial milestones and tiered royalties."

Licensing / partnership • New trial • Solid Tumor

An Investigational Study of BGB-58067 in Participants With Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=92 | Recruiting | Sponsor: BeiGene | Not yet recruiting ➔ Recruiting

Enrollment open • Metastases • Oncology • Solid Tumor

BeiGene's PRMT5 inhibitor BGB-58067 clinical trial application accepted, leading the way in anti-cancer treatment [Google translation] (pharnexcloud.com) - "On September 10, according to the official website of the CDE, BeiGene 's application for clinical trial of BGB-58067 tablets, a Class 1 new drug, was accepted. According to the company's public information, BGB-58067 is a PRMT5 inhibitor and a solid tumor product under development by BeiGene, which is expected to enter the clinical research stage in 2024...According to BeiGene's public information, the MTA-synergistic PRMT5 inhibitor developed by the company is highly effective and selective, and has brain penetration, and is expected to be used for solid tumors such as non-small cell lung cancer and gastrointestinal tumors."

New trial • Gastrointestinal Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

An Investigational Study of BGB-58067 in Participants With Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=92 | Not yet recruiting | Sponsor: BeiGene

Metastases • New P1 trial • Oncology • Solid Tumor