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Merestinib

Phase 1

Advanced Cancer | Small molecule | Oncology |Eli Lilly and Company|Last Updated: May 19, 2020

Target and mechanism

Molecular targetMET
Target classInhibitor
ModalitySmall molecule

Success Probability

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Market & Valuation

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Trial Design

CONTROLLED
Total Trials1
Total Enrollment19

FDA Designations

No designations recorded

Clinical trial landscape

Merestinib · 2 trials · 8 indications

Phase 1 2
NCT03027284A Study of Merestinib (LY2801653) in Japanese Participants With Advanced or Metastatic CancerAdvanced Cancer
COMPLETED19 Analytics
NCT02779738A Study of Merestinib (LY2801653) in Healthy ParticipantsHealthy
COMPLETED24 Analytics
PHASE1COMPLETED
A Study of Merestinib (LY2801653) in Japanese Participants With Advanced or Metastatic Cancer
Advanced CancerUnlock trial analytics
PHASE1COMPLETED
A Study of Merestinib (LY2801653) in Healthy Participants
HealthyUnlock trial analytics

Study Endpoints

Primary Endpoints

Number of Participants with Merestinib Dose-Limiting Toxicities (DLTs)
Cycle 1 (Part A = 28 Days or Part B = 21 Days)

Number of participants with DLTs

Pharmacokinetics (PK): Maximum Concentration (Cmax) for Merestinib for High-Fat Meal and Fasted State
Predose through 120 hours after administration of study drug
Pharmacokinetics: Maximum Concentration (Cmax) for Merestinib for Standard Meal and Fasted State
Predose through 120 hours after administration of study drug
Pharmacokinetics: Area Under The Concentration Curve AUC(0-∞) for Merestinib for High-Fat Meal and Fasted State
Predose through 120 hours after administration of study drug
Pharmacokinetics: Area Under The Concentration Curve AUC(0-∞) for Merestinib for Standard Meal and Fasted State
Predose through 120 hours after administration of study drug

Secondary Endpoints

Pharmacokinetics (PK): Maximum Concentration (Cmax) of Merestinib and its Metabolites
Predose Cycle 1 Throughout the First 2 Cycles (Part A = 28-Day Cycles, Part B = 21-Day Cycles)
PK: Area Under the Concentration Time Curve (AUC) of Merestinib and its Metabolites
Predose Cycle 1 Throughout the First 2 Cycles (Part A = 28-Day Cycles, Part B = 21-Day Cycles)
Objective Response Rate (ORR): Percentage of Participants With a Complete or Partial Response
Baseline to Measured Progressive Disease or Start of New Anti-Cancer Therapy (Estimated as up to 8 Months)
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Study Design & Arms

AllocationNON_RANDOMIZED
MaskingNONE
ModelSINGLE_GROUP
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
Merestinib (Part A Dose Level 1)EXPERIMENTALMerestinib administered orally. Treatment will continue until disease progression, development of unacceptable toxicity, or other discontinuation criteria are met.
Merestinib (Part A Dose Level 2)EXPERIMENTALMerestinib administered orally. Treatment will continue until disease progression, development of unacceptable toxicity, or other discontinuation criteria are met.
Merestinib + Cisplatin + Gemcitabine (Part B)EXPERIMENTALMerestinib administered orally with cisplatin and gemcitabine administered intravenously (IV). Treatment will continue until disease progression, development of unacceptable toxicity, or other discontinuation criteria are met, but Cisplatin and gemcitabine treatment will be limited to a maximum of 8 cycles.
Merestinib FastedEXPERIMENTALSingle dose of merestinib administered in fasted state in one of three periods
Merestinib Standard MealEXPERIMENTALSingle dose of merestinib administered with a standard meal in one of three periods
Merestinib High-Fat MealEXPERIMENTALSingle dose of merestinib administered with a high-fat meal in one of three periods

Interventions

NameTypeDescription
MerestinibDRUGAdministered orally
CisplatinDRUGAdministered IV
GemcitabineDRUGAdministered IV
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Eligibility Criteria

Age Range20 Years to N/A
SexALL
Healthy VolunteersNo
Study Sites2

Inclusion Criteria: * Part A: Histological or cytological evidence of a diagnosis of cancer that is advanced and/or metastatic (solid tumors or non-Hodgkin's lymphoma). * Part B: Biliary tract carcinoma that is unresectable, recurrent, or metastatic. The participant must not have received prior sys...

Countries:JapanUnited States
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Competitive Landscape -Cancer 5 trials (matched to "Advanced Cancer")

Frequently asked questions about Merestinib

What is Merestinib used for?

Merestinib is an investigational small molecule being studied for use in healthy participants and in patients with advanced or metastatic cancer, including biliary tract carcinoma, cholangiocarcinoma, gall bladder carcinoma, solid tumors, and non-Hodgkin's lymphoma. It is in Phase 1 clinical development and is not approved by the FDA.

What does Merestinib target?

Merestinib targets MET, a receptor tyrosine kinase, and acts as an inhibitor of this target. By inhibiting MET, the drug is designed to interfere with signaling pathways that can promote tumor growth and progression in certain cancers.

Who makes Merestinib?

Merestinib is being developed by Eli Lilly and Company, a pharmaceutical company traded on the New York Stock Exchange under the ticker symbol LLY. The company is conducting clinical trials to evaluate the drug's safety and tolerability in humans.

What phase is Merestinib in?

Merestinib is in Phase 1 clinical development. It has completed two Phase 1 trials, one in healthy participants and one in Japanese participants with advanced or metastatic cancer. The drug remains investigational and has not received FDA approval.

What clinical trials is Merestinib in?

Merestinib has completed two Phase 1 clinical trials. The first, NCT02779738, enrolled 24 healthy participants in the United States. The second, NCT03027284, enrolled 19 Japanese participants with advanced or metastatic cancer, including biliary tract carcinoma and solid tumors.

Is Merestinib the same as LY2801653?

Yes, Merestinib is also known as LY2801653. Both names refer to the same investigational drug, and clinical trial records use the LY2801653 designation. Researchers and investors may encounter either name in publications and trial databases.