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OP-3136

Phase 1

Advanced or Metastatic ER+ HER2- Breast Cancer (mBC) | Small molecule | Oncology |Olema Pharmaceuticals, Inc.|Last Updated: Oct 10, 2025

Target and mechanism

Molecular targetKAT6
Target classLysine Acetyltransferase
ModalitySmall molecule

Success Probability

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Market & Valuation

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Trial Design

RandomizedCONTROLLED
Total Trials1
Total Enrollment180

FDA Designations

No designations recorded

Clinical trial landscape

OP-3136 · 1 trial · 6 indications

Phase 1 1
NCT06784193Phase 1 Study of OP-3136 in Advanced or Metastatic Solid TumorsAdvanced or Metastatic ER+ HER2- Breast Cancer (mBC)
RECRUITING180 Analytics
PHASE1RECRUITING
Phase 1 Study of OP-3136 in Advanced or Metastatic Solid Tumors
Advanced or Metastatic ER+ HER2- Breast Cancer (mBC)Unlock trial analytics

Study Endpoints

Primary Endpoints

Number of participants with dose-limiting toxicities in the Dose Escalation Arms
Up to 28 days
Incidence of adverse events and laboratory abnormalities
Up to 26 months

Secondary Endpoints

Maximum observed concentration (Cmax)
Up to 26 months
Time to maximum concentration (Tmax)
Up to 26 months
Area under the curve from time zero to 24 hours (AUC0-24)
Up to 26 months
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Study Design & Arms

AllocationRANDOMIZED
MaskingNONE
ModelSEQUENTIAL
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
Part 1A Dose Escalation monotherapyEXPERIMENTAL -
Part 1B Dose Escalation in combination with fulvestrantEXPERIMENTAL -
Part 1C Dose Escalation in combination with palazestrantEXPERIMENTAL -
Part 2A Dose Expansion monotherapy - mBCEXPERIMENTAL -
Part 2A Dose Expansion monotherapy - mCRPCEXPERIMENTAL -
Part 2B Dose Expansion in combination with fulvestrant OR palazestrant-mBC @ RDE 1EXPERIMENTAL -
Part 2B Dose Expansion in combination with fulvestrant OR palazestrant-mBC @ RDE 2EXPERIMENTAL -

Interventions

NameTypeDescription
OP-3136DRUGSelective inhibitor of HAT enzymes KAT6A and KAT6B
FulvestrantDRUGSelective estrogen receptor degrader (SERD)
PalazestrantDRUGComplete estrogen receptor antagonist (CERAN)
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Eligibility Criteria

Age Range18 Years to N/A
SexALL
Healthy VolunteersNo
Study Sites8

Key Inclusion Criteria: * Participants with advanced or metastatic ER+HER2- breast cancer, mCRPC, or NSCLC (Part 1) or advanced or metastatic ER+HER2- BC or mCRPC (Part 2). * Part 1A (Dose escalation for OP-3136 monotherapy): Participants must have a tumor that is unresectable or metastatic and for...

Countries:United StatesAustralia
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Competitive Landscape -Breast Cancer 402 trials (matched to "Advanced or Metastatic ER+ HER2- Breast Cancer (mBC)")

Top 20 of 92 competitors

CompanyTickerTrialsLead PhaseDrugs
AstraZeneca PLCAZN47PHASE3Fulvestrant, Capivasertib
Merck & Co., Inc.MRK12PHASE3Pembrolizumab, Paclitaxel, Doxorubicin, Epirubicin, Cyclophosphamide
Eli Lilly and CompanyLLY27PHASE3Abemaciclib, Standard Adjuvant Endocrine Therapy
BioNTech SE Sponsored ADRBNTX7PHASE3DB-1303/BNT323, T-DM1
Gilead Sciences, Inc.GILD13PHASE3Sacituzumab Govitecan-hziy, Eribulin, Capecitabine Product, Gemcitabine, Vinorelbine
Novartis AG Sponsored ADRNVS30PHASE3Ribociclib
Pfizer Inc.PFE34PHASE3ARV-471, Fulvestrant
BeOne Medicines Ltd. Sponsored ADRONC5PHASE3BGB-43395, Letrozole, Abemaciclib, Palbociclib, Ribociclib
Olema Pharmaceuticals, Inc.OLMA5PHASE3Palazestrant, Fulvestrant, Anastrozole, Letrozole, Exemestane
Jazz Pharmaceuticals Public Limited CompanyJAZZ3PHASE3Zanidatamab, Trastuzumab, Eribulin, Vinorelbine, Gemcitabine
Celcuity Inc.CELC3PHASE3Gedatolisib, Palbociclib, Fulvestrant, Alpelisib
Relay Therapeutics, Inc.RLAY2PHASE3Zovegalisib, Capivasertib, Fulvestrant
GSK plc Sponsored ADRGSK2PHASE3Niraparib
Greenwich LifeSciences, Inc.GLSI1PHASE3GLSI-100
Bristol-Myers Squibb CompanyBMY5PHASE2Iza-bren, Nab-paclitaxel, Paclitaxel, Capecitabine, Carboplatin
BriaCell Therapeutics CorpBCTX2PHASE3SV-BR-1-GM, Cyclophosphamide, Interferon infiltration of the inoculation site, Retifanlimab, Treatment of Physician's Choice
Incyte CorporationINCY4PHASE2Ruxolitinib, Capecitabine, Regorafenib
Natera, Inc.NTRA3PHASE2Discontinuation of the anti-HER2 maintenance therapy
Puma Biotechnology, Inc.PBYI3PHASE2Neratinib, Loperamide, Colesevelam
Atossa Therapeutics, Inc.ATOS1PHASE2endoxifen, goserelin
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Frequently asked questions about OP-3136

What is OP-3136 used for?

OP-3136 is an investigational small molecule being developed for the treatment of advanced or metastatic ER+ HER2- breast cancer (mBC). It is also being studied in advanced or metastatic non-small cell lung cancer (NSCLC) and castration-resistant prostate cancer (mCRPC). The drug is currently in Phase 1 clinical development.

What does OP-3136 target?

OP-3136 targets KAT6, a lysine acetyltransferase enzyme. By inhibiting KAT6, the drug may affect gene expression pathways involved in tumor growth. This mechanism is being evaluated in a Phase 1 study for advanced or metastatic solid tumors, including ER+ HER2- breast cancer.

Who makes OP-3136?

OP-3136 is being developed by Olema Pharmaceuticals, Inc., a biopharmaceutical company traded on the NASDAQ under the ticker symbol OLMA. The company is conducting a Phase 1 clinical trial of OP-3136 in patients with advanced or metastatic solid tumors.

What phase is OP-3136 in?

OP-3136 is in Phase 1 clinical development. It is an investigational drug and has not been approved by the FDA. The ongoing Phase 1 study is recruiting participants to evaluate the safety, tolerability, and preliminary efficacy of OP-3136 in advanced or metastatic solid tumors.

What clinical trials is OP-3136 in?

OP-3136 is being studied in a Phase 1 clinical trial with the identifier NCT06784193. This trial is recruiting 180 participants with advanced or metastatic ER+ HER2- breast cancer, non-small cell lung cancer, or castration-resistant prostate cancer. The study is being conducted in the United States and Australia.

Is OP-3136 the same as palazestrant?

OP-3136 is not the same as palazestrant. Palazestrant is listed as a condition or treatment in the clinical trial for OP-3136, indicating it may be used as a combination agent or comparator in the study. OP-3136 is a distinct investigational drug targeting KAT6.