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Encorafenib formulation

Phase 1

Healthy | Small molecule | Other |Pfizer, Inc.|Last Updated: Feb 23, 2024

Target and mechanism

Molecular targetBRAF
Target classInhibitor
ModalitySmall molecule

Also known as Encorafenib

Success Probability

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Market & Valuation

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Trial Design

RandomizedCONTROLLED
Total Trials1
Total Enrollment18

FDA Designations

No designations recorded

Clinical trial landscape

Encorafenib formulation · 1 trial · 1 indication

Phase 1 1
NCT05446142A Relative Bioavailability Study Evaluating Two New Encorafenib FormulationsHealthy
COMPLETED18 Analytics
PHASE1COMPLETED
A Relative Bioavailability Study Evaluating Two New Encorafenib Formulations
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Study Endpoints

Primary Endpoints

Area Under the Plasma Concentration-Time Profile From Time Zero to Extrapolated Infinite Time (AUCinf) Following Single Oral Doses of Encorafenib 75 mg Alone and With Rabeprazole
Day 1 predose, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 24, 48 hours postdose

AUCinf for encorafenib eMCC, eMCCL and CAP formulations (75 mg, single dose administration), and for encorafenib eMCC and eMCCL formulations (75 mg, single dose administration) following 5 days of rabeprazole 20 mg daily were calculated by AUClast + (Clast/kel), where AUClast was the area under the plasma concentration-time profile from time zero to last quantifiable concentration, Clast was the predicted plasma concentration at the last quantifiable time point estimated from the log-linear regression analysis, and kel was first-order elimination rate constant.

Maximum Observed Plasma Concentration (Cmax) Following Single Oral Doses of Encorafenib 75 mg Alone and With Rabeprazole
Day 1 predose, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 24, 48 hours postdose

Cmax for encorafenib eMCC, eMCCL and CAP formulations (75 mg, single dose administration), and for encorafenib eMCC and eMCCL formulations (75 mg, single dose administration) following 5 days of rabeprazole 20 mg daily were observed directly from data.

Area Under the Plasma Concentration-Time Profile From Time Zero to Last Quantifiable Concentration (AUClast) Following Single Oral Doses of Encorafenib 75 mg Alone and With Rabeprazole
Day 1 predose, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 24, 48 hours postdose

AUClast for encorafenib eMCC, eMCCL and CAP formulations (75 mg, single dose administration), and for encorafenib eMCC and eMCCL formulations (75 mg, single dose administration) following 5 days of rabeprazole 20 mg daily were calculated using Linear/Log trapezoidal method.

Secondary Endpoints

Time for Cmax (Tmax) Following Single Oral Doses of Encorafenib 75 mg Alone and With Rabeprazole
Day 1 predose, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 24, 48 hours postdose
Terminal Half-Life (t½) Following Single Oral Doses of Encorafenib 75 mg Alone and With Rabeprazole
Day 1 predose, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 24, 48 hours postdose
Apparent Clearance (CL/F) Following Single Oral Doses of Encorafenib 75 mg Alone and With Rabeprazole
0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 10, 12, 24, 48 hours postdose
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Study Design & Arms

AllocationRANDOMIZED
MaskingNONE
ModelCROSSOVER
PurposeOTHER

Treatment Arms

ArmTypeDescription
Four Period Treatment Sequence: PPI EffectEXPERIMENTALParticipants will receive a single encorafenib dose formulation, a single encorafenib dose of the formulated capsule (CAP), and a single encorafenib dose of the formulation after administration of 20 mg rabeprazole every evening for 5 days.
Four Period Treatment Sequence: PPI Effect Second FormulationEXPERIMENTALParticipants will receive a single encorafenib dose of the second formulation, a single encorafenib dose of the second formulation, a single encorafenib dose of the formulated capsule (CAP), and a single encorafenib dose of the second formulation after administration of 20 mg rabeprazole every evening for 5 days.

Interventions

NameTypeDescription
Encorafenib capsule formulation (CAP)DRUGA single encorafenib dose of the CAP formulation
Encorafenib first formulationDRUGfirst formulation
Encorafenib second formulationDRUGsecond formulation
Rabeprazole tabletDRUGProton-pump inhibitor
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Eligibility Criteria

Age Range18 Years to N/A
SexALL
Healthy VolunteersYes
Study Sites1

Inclusion Criteria: * Participants must be male or female of non-childbearing potential of 18 years of age or older, inclusive, at the time of signing the informed consent document. * Male and female participants who are overtly healthy as determined by medical evaluation including medical history,...

Countries:United States
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Frequently asked questions about Encorafenib formulation

What is Encorafenib used for?

Encorafenib is an investigational small molecule being studied for the treatment of cancers including metastatic colorectal cancer, melanoma, and solid tumors harboring a BRAF V600 mutation. It is in Phase 3 clinical development for these oncology indications.

How does Encorafenib work?

Encorafenib is a kinase inhibitor, belonging to the -nib class of drugs. It targets and inhibits BRAF kinases, which are involved in cell growth and proliferation. By blocking these kinases, Encorafenib aims to slow or stop the growth of cancer cells that harbor BRAF mutations.

Who is developing Encorafenib?

Encorafenib is being developed by Pfizer, Inc., a biopharmaceutical company traded on the New York Stock Exchange under the ticker symbol PFE. The company is conducting clinical trials to evaluate the drug's safety and efficacy in various cancer indications.

What phase is Encorafenib in?

Encorafenib is in Phase 3 clinical development. It is an investigational drug and has not been approved by regulatory authorities. Its safety and efficacy are still being evaluated in ongoing and completed clinical trials.

What clinical trials is Encorafenib in?

Encorafenib has been studied in several clinical trials, including NCT01909453, a Phase 3 trial in BRAF mutant melanoma; NCT02159066, a Phase 2 trial in advanced BRAF melanoma; NCT02928224, a Phase 3 trial in BRAF V600E-mutant metastatic colorectal cancer; and NCT04657991, an active Phase 3 trial in advanced or metastatic melanoma.

Is Encorafenib the same as LGX818?

Yes, Encorafenib is also known as LGX818. Clinical trial titles and protocols often refer to the drug by this alternative name, such as in studies combining LGX818 with other agents for the treatment of BRAF-mutant cancers.