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LY2801653

Phase 2

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

LY2801653 development status

Highest phase Phase 2 (NCT02711553)
Phase scored for LLYPhase 1
Registered trials 8 across 2 sponsors since Jan 2011

LY2801653 target and mechanism

ModalitySmall molecule

Also known as [^14C]-LY2801653, Merestinib

Success Probability

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Market & Valuation

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Trial Design

UNCONTROLLED
Total Trials2
Total Enrollment209

FDA Designations

No designations recorded

LY2801653 clinical trials

LY2801653 · 2 trials · 8 indications

Phase 1 2
NCT03027284A Study of Merestinib (LY2801653) in Japanese Participants With Advanced or Metastatic CancerAdvanced Cancer
COMPLETED19 Analytics
NCT01285037A Study of LY2801653 in Advanced CancerCancer
COMPLETED190 Analytics
PHASE1COMPLETED
A Study of Merestinib (LY2801653) in Japanese Participants With Advanced or Metastatic Cancer
Advanced CancerUnlock trial analytics
PHASE1COMPLETED
A Study of LY2801653 in Advanced Cancer
CancerUnlock 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

Recommended dose for phase 2 studies: Maximum tolerated dose
Baseline to study completion (estimated as 3 months)

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.
LY2801653EXPERIMENTALThis study consists of a dose escalation of LY2801653 (Part A) followed by dose confirmation cohorts in four tumor types (adenocarcinoma of the colon or rectum, head and neck squamous cell carcinoma, uveal melanoma with liver metastasis, and cholangiocarcinoma) (Part B). Part C consists of dose determination for LY2801653 in combination with cetuximab in participants with head and neck squamous cell carcinoma followed by an expansion cohort. Part D consists of dose determination for LY2801653 in combination with cisplatin in participants with cholangiocarcinoma followed by an expansion cohort. Part E consists of dose determination for LY2801653 in combination with gemcitabine and cisplatin. Part F consists of dose determination for LY2801653 in combination with ramicirumab.

Interventions

NameTypeDescription
MerestinibDRUGAdministered orally
CisplatinDRUGAdministered IV
GemcitabineDRUGAdministered IV
LY2801653DRUGLY2801653 given orally once daily during 28-day cycles. Participants may continue on study drug until disease progression, unacceptable toxicity, or other withdrawal criterion is met.
CetuximabDRUGCetuximab given via IV infusion once weekly, 400mg/m2 for first dose and 250mg /m2 for subsequent doses. If LY2801653 treatment is stopped due to toxicity after a minimum of 4 cycles, cetuximab may be continued until disease progression. In the event cetuximab treatment is stopped, participants may continue on study drug until disease progression, unacceptable toxicity, or other withdrawal criterion is met.
RamucirumabDRUGRamucirumab given via IV infusion every 2 weeks in a 28-day treatment cycle. Treatment with ramucirumab may continue until excessive toxicity or evidence of disease progression. In the absence of disease progression, treatment with LY2801653 may continue even if ramucirumab is discontinued provided no dose limiting toxicity related to LY2801653 is present. In the event that LY2801653 is discontinued, treatment with ramucirumab may be continued if there is no dose limiting toxicity related to ramucirumab.
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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 7 trials

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Frequently asked questions about LY2801653

What is LY2801653?

LY2801653 is an investigational small molecule being developed by Eli Lilly and Company for the treatment of advanced cancer. It has been studied in a Phase 1 clinical trial and is not yet approved for any indication.

What is LY2801653 used for?

LY2801653 is being studied for use in cancer. It was evaluated in a Phase 1 trial in patients with advanced cancer. It is investigational and has not been approved for any use.

Who is developing LY2801653?

LY2801653 is being developed by Eli Lilly and Company, which trades on the New York Stock Exchange under the ticker symbol LLY.

What phase is LY2801653 in?

LY2801653 is in Phase 1 clinical development. It has completed one Phase 1 trial in advanced cancer and is not approved for any indication.

What clinical trials is LY2801653 in?

LY2801653 has been studied in one clinical trial: NCT01285037, titled "A Study of LY2801653 in Advanced Cancer." This Phase 1 trial was completed and enrolled 190 participants in the United States.

Is LY2801653 the same as [^14C]-LY2801653?

Yes, [^14C]-LY2801653 is an alternative name for LY2801653. Both refer to the same investigational small molecule developed by Eli Lilly and Company for cancer.