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Mervometostat

Phase 1

Metastatic Castration Resistant Prostate Cancer (mCRPC) | Small molecule | Oncology |Pfizer, Inc.|Last Updated: Aug 24, 2026

Target and mechanism

Target class-Stat (Enzyme)
ModalitySmall molecule

Also known as PF-06821497, Mervometostat (PF-06821497), Mevrometostat

Success Probability

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Market & Valuation

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Trial Design

CONTROLLED
Total Trials1
Total Enrollment453

FDA Designations

No designations recorded

Clinical trial landscape

Mervometostat · 1 trial · 3 indications

Phase 1 1
NCT03460977A Study of Mevrometostat for Treatment of Relapsed/Refractory SCLC, Castration Resistant Prostate Cancer, and Follicular LymphomaMetastatic Castration Resistant Prostate Cancer (mCRPC)
RECRUITING453 Analytics
PHASE1RECRUITING
A Study of Mevrometostat for Treatment of Relapsed/Refractory SCLC, Castration Resistant Prostate Cancer, and Follicular Lymphoma
Metastatic Castration Resistant Prostate Cancer (mCRPC)Unlock trial analytics

Study Endpoints

Primary Endpoints

Percentage of patients with dose limiting toxicities (DLTs) to determine the maximum tolerated dose (MTD)
Baseline up to 90 days

First cycle DLTs will be utilized to determine the MTD

Overall safety profile including adverse events
Baseline up to approximately 2 years

Adverse Events will be graded by National Cancer Institute Common Terminology Criteria for Adverse Events (NCI CTCAE version \[4.03\])

Preliminary efficacy determination as evaluated by disease specific response criteria
Through study completion, approximately 2 years past last patient first visit.

Objective response using Response Evaluation Criteria in Lymphoma (RECIL) for lymphoma, Response Evaluation Criteria in Solid Tumors (RECIST) 1.1 for solid tumors including Small Cell Lung Cancer (SCLC) and Prostate Cancer Working Group 3 (PCWG3) for Castration Resistant Prostate Cancer (CRPC). Progression-free survival in Part 2B in patients with CRPC.

Overall safety profile including laboratory abnormalities
Baseline up to approximately 2 years

Laboratory abnormalities as characterized by type, frequency, severity (as graded by NCI CTCAE version \[4.03\]), and timing.

Overall safety profile including vital signs
Baseline up to approximately 2 years

Vital sign changes from baseline including blood pressure, heart rate, ECG changes.

Evaluate time to event mevrometostat and enzalutamide vs enzalutamide alone including radiographic prgression free survival
Baseline until disease progression or death or through study completion (approx 2 years)

PCWG3

Secondary Endpoints

Evaluate time to event anti-tumor activity of mevrometostat including progression-free survival (PFS), PSA50, Duration of Response (DoR), Time to first skeletal related event and Time to symptomatic skeletal related event, depending on tumor type.
Baseline and every 21 days through time of confirmed disease progression, unacceptable toxicity, or through study completion, approximately 2 years.
Evaluate overall survival
Baseline up to approximately 2 years
Pharmacokinetic Parameters: Maximum Observed Plasma Concentration (Cmax)
At specific timepoints from Cycle 1 day 1 to End of Treatment visit
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Study Design & Arms

AllocationNON_RANDOMIZED
MaskingNONE
ModelSEQUENTIAL
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
Dose Escalation (Part 1A)EXPERIMENTALParticipants with SCLC, CRPC and FL will receive mevrometostat at escalating dose levels
Dose Escalation (Part 1B)EXPERIMENTALParticipants with FL will receive mevrometostat at escalating dose levels
Dose Escalation (Part 1C)EXPERIMENTALParticipants with mCRPC will receive mevrometostat at escalating dose levels.
Dose Escalation (Part 2A)EXPERIMENTALParticipants with mCRPC and SCLC will receive mevrometostat at escalating dose levels in combination with SOC.
Dose Expansion (Part 2B)EXPERIMENTALParticipants with CRPC will receive mevrometostat in combination with SOC or SOC alone.
Japan CohortEXPERIMENTALParticipants with CRPC will receive mevrometostat at one or two doses
China cohortEXPERIMENTALParticipants will receive mevrometostat at one or two doses
Dose Expansion (Part 2C)EXPERIMENTALParticipants with mCRPC will receive mevrometostat at a different dose/dosing regimen than that of Part 2B in combination with SOC
BE SubstudyEXPERIMENTALIn the assessment phase, each enrolled participant will receive single doses of the 2 different mevrometostat formulations in 3 periods with alternating dosing and washout between each dose. In the maintenance phase, each participant will receive mevrometostat 2 times a day and enzalutamide 1 time a day.
DDI SubstudyEXPERIMENTALThe DDI substudy assessment phase will consist of 2 Cohorts, Cohort 1 (monotherapy cohort) and Cohort 2 (combination cohort). In the Cohort 1 assessment phase, each enrolled participant will receive a combination of mevrometostat and itraconazole based on preset schedule. In the Cohort 2 assessment phase, each enrolled participant will receive a combination of mevrometostat, enzalutamide, and itraconazole based on preset schedule. In the maintenance phase, each participant will receive mevrometostat 2 times a day and enzalutamide 1 time a day.

Interventions

NameTypeDescription
Mervometostat (PF-06821497)DRUGOral continuous
EnzalutamideDRUGOral continuous
ItraconazoleDRUGOral solution
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Eligibility Criteria

Age Range18 Years to N/A
SexALL
Healthy VolunteersNo
Study Sites84

Part 1 and Part 2 (Closed for enrollment). Part 3 Key Inclusion Criteria: * Histological or cytological diagnosis of castration resistant prostate cancer. * Eastern Cooperative Oncology Group (ECOG) Performance Status (PS) of 0-2 with expected life expectancy of at least 6 months. * Adequate bone ...

Countries:United StatesBulgariaChinaJapanPolandRussiaSouth KoreaSpain
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Recent Changes (Last 90 Days)

LOWAug 24, 2026NCT03460977lastUpdatePostDate: changed
LOWAug 24, 2026NCT03460977lastUpdatePostDate: changed
LOWJul 29, 2026NCT03460977lastUpdatePostDate: changed
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LOWJul 9, 2026NCT03460977lastUpdatePostDate: changed
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LOWJul 2, 2026NCT03460977lastUpdatePostDate: changed
LOWJul 2, 2026NCT03460977lastUpdatePostDate: changed
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LOWJun 16, 2026NCT03460977lastUpdatePostDate: changed
LOWJun 16, 2026NCT03460977lastUpdatePostDate: changed
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Frequently asked questions about Mervometostat

What is Mervometostat used for?

Mervometostat is an investigational small molecule being developed by Pfizer for metastatic castration-resistant prostate cancer (mCRPC) and metastatic castration-sensitive prostate cancer (mCSPC). It is also being studied in healthy participants to understand how the drug is processed by the body.

How does Mervometostat work?

Mervometostat is a small molecule enzyme inhibitor, classified under the -stat (enzyme) target class. It is being studied to treat prostate cancer by targeting specific enzymes involved in cancer growth, though the exact molecular target is not disclosed in the available information.

Who makes Mervometostat?

Mervometostat is developed by Pfizer, Inc., a biopharmaceutical company listed on the New York Stock Exchange under the ticker symbol PFE. The drug is also known by the code name PF-06821497.

What phase is Mervometostat in?

Mervometostat is in Phase 1 clinical development for metastatic castration-resistant prostate cancer and metastatic castration-sensitive prostate cancer. It is also being studied in healthy participants. The drug is investigational and has not been approved by regulatory authorities.

What clinical trials is Mervometostat in?

Mervometostat is being studied in several clinical trials. NCT03460977 is a Phase 1 trial in mCRPC, small cell lung cancer, and follicular lymphoma. NCT06392230 is a completed Phase 1 trial in healthy participants. NCT06629779 is a Phase 3 trial in mCRPC, and NCT07028853 is a Phase 3 trial in mCSPC.

Is Mervometostat the same as PF-06821497?

Yes, Mervometostat is also known as PF-06821497. The drug is referred to by both names in clinical trial registries and scientific literature, with PF-06821497 being the code name used during early development.