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BGB-58067

Phase 1

Advanced Solid Tumor | Small molecule | Oncology |BeOne Medicines Ltd.|Last Updated: Aug 10, 2026

Target and mechanism

Molecular targetPRMT5
Target classProtein
ModalitySmall molecule

Also known as BGB-58067 Tablet (F-01 Formulation)

Success Probability

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Market & Valuation

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Trial Design

CONTROLLED
Total Trials1
Total Enrollment525

FDA Designations

No designations recorded

Clinical trial landscape

BGB-58067 · 4 trials · 3 indications

Phase 1 3Early Phase 1 1
NCT07712640A Study to Investigate the Relative Bioavailability of 2 Tablet Formulations and the Effect of Food on the Pharmacokinetics of BGB-58067 in Healthy ParticipantsHealthy Volunteers
RECRUITING32 Analytics
NCT07590102A Study to Investigate the Effect of the CYP3A Inducer Phenytoin and the CYP3A Inhibitor Itraconazole on the Pharmacokinetics of BGB-58067 in Healthy ParticipantsHealthy Volunteers
RECRUITING30 Analytics
NCT06589596An Investigational Study of BGB-58067 As a Single Agent and in Combination With Anticancer Agents in Participants With Advanced Solid TumorsAdvanced Solid Tumor
RECRUITING525 Analytics
PHASE1RECRUITING
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
Healthy VolunteersUnlock trial analytics
PHASE1RECRUITING
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
Healthy VolunteersUnlock trial analytics
PHASE1RECRUITING
An Investigational Study of BGB-58067 As a Single Agent and in Combination With Anticancer Agents in Participants With Advanced Solid Tumors
Advanced Solid TumorUnlock trial analytics

Study Endpoints

Primary Endpoints

Area under the Plasma Concentration-Time Curve from Time 0 Infinity (AUC0-inf) for BGB-58067
Approximately 4 Days
Area under the Plasma Concentration-Time Curve from Time 0 to the Time of the Last Quantifiable Concentration (AUC0-t last) for BGB-58067
Approximately 4 Days
Maximum Observed Plasma Concentration (Cmax) of BGB-58067
Approximately 4 Days
Time of the Maximum Observed Concentration (Tmax) for BGB-58067
Approximately 4 Days
Apparent Terminal Elimination Half-life (t1/2) for BGB-58067
Approximately 4 Days
Apparent Total Clearance from Plasma after Oral Administration (CL/F) for BGB-58067
Approximately 4 Days
Apparent Volume of Distribution at Steady State after Extravascular Administration (Vz/F) for BGB-58067
Approximately 4 Days
Part A and Part B: Time of the Maximum Observed Concentration (Tmax) of BGB-58067
Part A: Day 1 and Day 18; Part B: Day 1 and Day 8
Part A and Part B: Maximum Observed Concentration (Cmax) of BGB-58067
Part A: Day 1 and Day 18; Part B: Day 1 and Day 8
Part A and Part B: Area Under the Concentration-time Curve from Time 0 to the Time of the Last Quantifiable Concentration (AUC0-last) of BGB-58067
Part A: Day 1 and Day 18; Part B: Day 1 and Day 8
Part A and Part B: Area Under the Concentration-time Curve from Time 0 Extrapolated to Infinity (AUC0-∞) of BGB-58067
Part A: Day 1 and Day 18; Part B: Day 1 and Day 8
Part A and Part B: Apparent Terminal Elimination Half-life (t1/2) of BGB-58067
Part A: Day 1 and Day 18; Part B: Day 1 and Day 8
Part A and Part B: Apparent Total Clearance (CL/F) of BGB-58067
Part A: Day 1 and Day 18; Part B: Day 1 and Day 8
Part A and Part B: Apparent Volume of Distribution During the Terminal Phase (Vz/F) of BGB-58067
Part A: Day 1 and Day 18; Part B: Day 1 and Day 8
Phase 1a: Number of Participants with Adverse Events and Serious Adverse Events
From first dose of the study drug(s) to 30 days after the last dose or initiation of a new anticancer therapy, whichever occurs first (approximately 13 months)

Number of participants with AEs and SAEs, including findings from physical examinations, electrocardiograms (ECGs), and laboratory assessments.

Phase 1a: Number of Participants with Adverse Events that meet Dose-Limiting Toxicity (DLT) criteria
Approximately 1 month
Phase 1a: Maximum Tolerated Dose (MTD) or Maximum Administered Dose (MAD) of BGB-58067 alone, in combination with BG-89894, and in combination with standard of care therapy
Approximately 1 month

MTD is defined as the highest dose evaluated for which estimated toxicity rate is the closest to the target toxicity rate. MAD is defined as the highest dose administered if MTD is not reached. Note: BGB-58067 + BG-89894 combination has been discontinued.

Phase 1a: Recommended Dose(s) for Expansion (RDFE[s]) of BGB-58067 alone, in combination with BG-89894, and in combination with standard of care therapy
Approximately 13 months

RDFE of BGB-58067 alone, in combination with BG-89894, and in combination with standard of care therapy will be determined based upon the MTD or MAD. Note: BGB-58067 + BG-89894 combination has been discontinued.

Phase 1b: Recommended Phase 2 Dose (RP2D) of BGB-58067 alone and in combination with standard of care therapy
Approximately 2 years

RP2D established from Phase 1a for BGB-58067 alone and in combination with standard of care therapy for administration in selected tumor types.

Phase 1b: Objective Response Rate (ORR)
Approximately 2 years

ORR is defined as the percentage of participants with confirmed complete response (CR) or partial response (PR), as assessed by the investigator.

Phase 0: Proportion of Participants with ≥ 50% Decrease from Baseline in SDMA Expression, or with SDMA H-Score ≤ 70, in Phase 0 Tumor Tissue Collected Intraoperatively
Intraoperatively

Decrease in SDMA expression in tumor tissue collected during Phase 0 surgery relative to baseline will be used if pre-treatment biopsy tissue is available. Otherwise, H-score ≤ 70 in tumor tissue collected during Phase 0 surgery will be used.

Phase 2: Proportion of Participants Alive at 12 Months
Date of Phase 0 surgery to date of death due to any cause, assessed up to 12 months

Overall survival at 12 months (OS12)

Secondary Endpoints

Number of Participants with Adverse Events (AEs)
Approximately 53 Days
Part A and Part B: Number of Participants with Adverse Events (AEs)
Up to approximately 30 days
Phase 1a: Objective Response Rate (ORR)
Approximately 2 years
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Study Design & Arms

AllocationRANDOMIZED
MaskingNONE
ModelCROSSOVER
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
Treatment Sequence 1EXPERIMENTALParticipants will receive a single oral dose of BGB-58067 F-01 tablet in fasted state, BGB-58067 F-02 tablet in fasted state, BGB-58067 F-02 tablet in the fed state with a high fat meal, and BGB-58067 F-02 tablet in the fed state with a low fat meal, with a 7-day washout between each dose.
Treatment Sequence 2EXPERIMENTALParticipants will receive a single oral dose of BGB-58067 F-02 tablet in fasted state, BGB-58067 F-02 tablet in the fed state with a low fat meal, BGB-58067 F-01 tablet in fasted state, and BGB-58067 F-02 tablet in the fed state with a high fat meal, with a 7-day washout between each dose.
Treatment Sequence 3EXPERIMENTALParticipants will receive a single oral dose of BGB-58067 F-02 tablet in fed state with low-fat meal, F-02 tablet in the fed state with a high fat meal, BGB-58067 F-02 tablet in fasted state, and BGB-58067 F-01 tablet in fasted state, with a 7-day washout between each dose.
Treatment Sequence 4EXPERIMENTALParticipants will receive a single oral dose of BGB-58067 F-02 tablet in fed state with high-fat meal, BGB-58067 F-01 tablet in fasted state, BGB-58067 F-02 tablet in the fed state with a low fat meal, and BGB-58067 F-02 tablet in fasted state, with a 7-day washout between each dose.
Part A: BGB-58067 + Phenytoin (CYP3A Inducer)EXPERIMENTALParticipants will receive BGB-58067 on Day 1 and Day 18 and phenytoin on Days 4 to 20.
Part B: BGB-58067 + Itraconazole (CYP3A Inhibitor)EXPERIMENTALParticipants will receive BGB-58067 on Days 1 and 8 and itraconazole on Days 4 to 11.
Phase 1a: BGB-58067 Monotherapy Dose Escalation and Safety ExpansionEXPERIMENTALSequential cohorts of increasing dose levels of BGB-58067 as monotherapy will be evaluated.
Phase 1a: BGB-58067 + BG-89894 Combination Therapy Dose EscalationEXPERIMENTALSequential cohorts of increasing dose levels of BGB-58067 in combination with BG-89894 will be evaluated. Enrollment in this combination has been discontinued.
Phase 1a: BGB-58067 + Standard of Care Combination Therapy Dose EscalationEXPERIMENTALSequential cohorts of increasing dose levels of BGB-58067 in combination with standard of care therapy will be evaluated.
Phase 1b: Dose Expansion and OptimizationEXPERIMENTALRecommended Dose(s) for Expansion (RDFE\[s\]) of BGB-58067 alone and in combination with standard of care therapy will be evaluated for selected indications and regimen(s) based on emerging data.
Arm A: Unmethylated-MGMT GBM-BGB-58067 MonotherapyEXPERIMENTALParticipants with unmethylated-MGMT and MTAP-deleted GBM demonstrating a positive PD response after Phase 0 surgery.
Arm B: Methylated-MGMT GBM-BGB-58067 + TMZ Concurrent TherapyEXPERIMENTALParticipants with methylated-MGMT and MTAP-deleted GBM demonstrating a positive PD response after Phase 0 surgery.

Interventions

NameTypeDescription
BGB-58067 Tablet (F-01 Formulation)DRUGAdministered orally
BGB-58067 Tablet (F-02 Formulation)DRUGAdministered orally
BGB-58067DRUGAdministered orally
PhenytoinDRUGAdministered orally
ItraconazoleDRUGAdministered orally
BG-89894DRUGPlanned doses administered on specified days per protocol.
Standard of Care TherapyDRUGAdministered in accordance with relevant local guidelines and/or prescribing information.
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Eligibility Criteria

Age Range18 Years to 65 Years
SexALL
Healthy VolunteersYes
Study Sites1

Inclusion Criteria: * Participants must be 18 to 65 years of age, inclusive, at the time of signing the ICF. * Participants who are overtly healthy, as determined by the investigator or delegate through medical evaluation * Female participants must be of non-childbearing potential. Note: A woman is...

Countries:AustraliaUnited StatesBrazilChinaDenmarkFranceMalaysiaMoldovaSouth KoreaSpainThailand
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Competitive Landscape -Other Solid Tumors 9 trials (matched to "Advanced Solid Tumor")

Recent Changes (Last 90 Days)

LOWAug 11, 2026NCT07712640Status: NOT_YET_RECRUITING → RECRUITING
LOWAug 11, 2026NCT07712640Status: NOT_YET_RECRUITING → RECRUITING
LOWAug 11, 2026NCT07712640Status: NOT_YET_RECRUITING → RECRUITING
LOWJul 22, 2026NCT07590102lastUpdatePostDate: changed
LOWJul 22, 2026NCT06589596lastUpdatePostDate: changed
LOWJul 22, 2026NCT07590102lastUpdatePostDate: changed
LOWJul 22, 2026NCT06589596lastUpdatePostDate: changed
LOWJul 17, 2026NCT07712640NEW_TRIAL: changed
LOWJul 17, 2026NCT07712640NEW_TRIAL: changed
LOWJul 13, 2026NCT06589596lastUpdatePostDate: changed
LOWJul 13, 2026NCT06589596lastUpdatePostDate: changed
LOWJul 9, 2026NCT07590102lastUpdatePostDate: changed
LOWJul 9, 2026NCT07590102lastUpdatePostDate: changed
LOWJun 22, 2026NCT06589596lastUpdatePostDate: changed
LOWJun 22, 2026NCT06589596lastUpdatePostDate: changed
LOWJun 18, 2026NCT07590102Status: NOT_YET_RECRUITING → RECRUITING
LOWJun 18, 2026NCT07590102Status: NOT_YET_RECRUITING → RECRUITING
LOWJun 18, 2026NCT07590102Status: NOT_YET_RECRUITING → RECRUITING
LOWJun 18, 2026NCT07590102Status: NOT_YET_RECRUITING → RECRUITING

Frequently asked questions about BGB-58067

What is BGB-58067 used for?

BGB-58067 is an investigational small molecule being studied for advanced solid tumors, glioblastoma (GBM), and in healthy volunteers for pharmacokinetic studies. It is currently in Phase 1 clinical development and is not yet approved by regulatory authorities.

What does BGB-58067 target?

BGB-58067 targets PRMT5, a protein involved in cellular processes relevant to cancer. By inhibiting PRMT5, the drug aims to interfere with tumor cell growth, particularly in cancers with specific genetic alterations such as MTAP-deleted glioblastoma.

Who is developing BGB-58067?

BGB-58067 is being developed by BeOne Medicines Ltd., a biopharmaceutical company listed on the stock exchange under the ticker ONC. The company is conducting clinical trials to evaluate the drug's safety and efficacy in oncology indications.

What phase is BGB-58067 in?

BGB-58067 is in Phase 1 clinical development. It is being studied in early-phase trials for advanced solid tumors, glioblastoma, and healthy volunteer pharmacokinetic studies. The drug is investigational and has not received regulatory approval.

What clinical trials is BGB-58067 in?

BGB-58067 is being evaluated in several trials, including NCT06589596 for advanced solid tumors, NCT07485049 for glioblastoma with MTAP-deleted tumors, and NCT07590102 and NCT07712640 for healthy volunteer pharmacokinetic studies. All trials are in Phase 1.

Is BGB-58067 the same as BGB-58067 Tablet (F-01 Formulation)?

Yes, BGB-58067 Tablet (F-01 Formulation) is an alternative name for BGB-58067. The F-01 formulation refers to a specific tablet version being tested in bioavailability studies, while the drug itself is the same active pharmaceutical ingredient.