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MK-0752

Phase 1

Advanced Breast Cancer | Small molecule | Oncology |Merck & Company, Inc.|Last Updated: Jun 17, 2016

Target and mechanism

ModalitySmall molecule

Also known as MK0752, Comparator: MK0752, Notch Inhibitor

Success Probability

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Market & Valuation

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Trial Design

CONTROLLED
Total Trials1
Total Enrollment103

FDA Designations

No designations recorded

Clinical trial landscape

MK-0752 · 2 trials · 3 indications

Phase 1 2
NCT00803894A Clinical Study to Determine Biomarkers of Response to a Gamma Secretase InhibitorHealthy
COMPLETED30 Analytics
NCT00106145A Notch Signalling Pathway Inhibitor for Patients With Advanced Breast Cancer (0752-014)Advanced Breast Cancer
COMPLETED103 Analytics
PHASE1COMPLETED
A Clinical Study to Determine Biomarkers of Response to a Gamma Secretase Inhibitor
HealthyUnlock trial analytics
PHASE1COMPLETED
A Notch Signalling Pathway Inhibitor for Patients With Advanced Breast Cancer (0752-014)
Advanced Breast CancerUnlock trial analytics

Study Endpoints

Primary Endpoints

To evaluate the existing Notch response signature using plucked hair follicle profiling data from health young male volunteers given 1000 mg MK0752 and 350 mg MK0752.
8.5 hours post dose.
Safety and tolerability; MTD will be established
Day 1 to Day 28

Secondary Endpoints

Overall tumor/disease response will be evaluated using RECIST criteria, radiographic and clinical evaluations
radigraphic evaluation = every 56 days
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Study Design & Arms

AllocationRANDOMIZED
MaskingDOUBLE
ModelCROSSOVER
PurposeDIAGNOSTIC

Treatment Arms

ArmTypeDescription
AACTIVE_COMPARATORMK0752 1000 mg
BACTIVE_COMPARATORMK0752 350 mg
CPLACEBO_COMPARATORPlacebo
Part I - Arm 1EXPERIMENTAL -
Part II - Arm 1EXPERIMENTAL -
Part III - Arm 1EXPERIMENTAL -
Part IV - Arm 1EXPERIMENTAL -
Part V - Arm 1EXPERIMENTAL -

Interventions

NameTypeDescription
MK0752DRUGSingle dose MK0752 capsules, 1000 mg: there will be a 7-day washout period between treatments.
Comparator: MK0752.DRUGSingle dose MK0752 capsules, 350 mg: there will be a 7-day washout period between treatments.
Comparator: PlaceboDRUGSingle dose placebo capsules: there will be a 7-day washout period between treatments.
Comparator: MK0752, Notch InhibitorDRUGDose escalating beginning with rising dose levels of 300, 450, and 600 mg/day in a continuous dosing schedule.
Comparator: MK0752, Notch Inhibitor - 450 mgDRUGDose 450 mg capsules daily for 28 day cycles.
Comparator: MK0752, Notch Inhibitor - 3 days on, 4 offDRUGDose escalating in a repeating intermittent dosing schedule of 3 days on and 4 days off at rising dose levels of 450, 600, 800, 1000, 1200, and 1400 mg/day.
Comparator: MK0752, Notch Inhibitor - 1 day on, 6 offDRUGDose escalating in a repeating intermittent dosing schedule of 1 day on/6 days off at rising dose levels of 600, 900, 1200, 1500, 1800, 2400, 3200 mg/day once weekly and then increase at 33% increments.
Comparator: MK0752, Notch Inhibitor - 3 days on, 4 off 350 mgDRUGDose 350 mg capsules daily intermittent 3 days on/4 days off dosing. THIS DOSING SCHEDULE IS NO LONGER UNDER INVESTIGATION
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Eligibility Criteria

Age Range18 Years to 35 Years
SexMALE
Healthy VolunteersYes

Inclusion Criteria: * Patient is a male * Patient has no clinically significant abnormality on electrocardiogram performed * Patient agrees to not to consume apple juice, grapefruit or grapefruit products beginning 2 weeks prior to first dose of study drug and for the duration of the study * Patien...

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Competitive Landscape -Breast Cancer 399 trials (matched to "Advanced Breast Cancer")

Top 20 of 91 competitors

CompanyTickerTrialsLead PhaseDrugs
AstraZeneca PLCAZN46PHASE3Fulvestrant, 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 CorpBCTX1PHASE3SV-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 MK-0752

What is MK0752 used for?

MK0752 is an investigational small molecule being studied for advanced breast cancer and other solid tumors, as well as in healthy volunteers for biomarker research. It is a gamma secretase inhibitor that targets the Notch signaling pathway. The drug is not approved and remains in clinical development.

What does MK0752 target?

MK0752 targets the Notch signaling pathway as a gamma secretase inhibitor. By inhibiting gamma secretase, it blocks Notch pathway activation, which is implicated in cancer cell growth and survival. This mechanism is being explored in advanced breast cancer and other solid tumors.

Who makes MK0752?

MK0752 is being developed by Merck & Company, Inc., traded on the New York Stock Exchange under the ticker MRK. The company is conducting clinical trials to evaluate the drug's safety and efficacy in oncology indications.

What phase is MK0752 in?

MK0752 is in Phase 1 clinical development. It has completed two Phase 1 trials, one in advanced breast cancer and other solid tumors and another in healthy volunteers. The drug is investigational and has not received FDA approval.

What clinical trials is MK0752 in?

MK0752 has completed two Phase 1 trials. NCT00106145 enrolled 103 patients with advanced breast cancer and other solid tumors. NCT00803894 enrolled 30 healthy male volunteers to determine biomarkers of response. Both trials are completed, and no active trials are listed.

Is MK0752 the same as a Notch inhibitor?

MK0752 is a Notch inhibitor, specifically a gamma secretase inhibitor that blocks Notch signaling. It is being studied for its potential in treating advanced breast cancer and other solid tumors by targeting this pathway.