CompletedPhase 1

Bioavailability Study of Vemurafenib in Participants With BRAF^V600 Mutation-Positive Malignancies

Hungary6 participantsStarted 2015-08-13

Plain-language summary

The purpose of this study is to characterize the pharmacokinetics (PK) of a single intravenous (IV) infusion of 14C-labeled vemurafenib administered shortly after an oral dose of vemurafenib and following multiple oral doses of vemurafenib twice daily (BID) at steady state as well as to estimate the absolute bioavailability of multiple oral doses of vemurafenib BID at steady state in participants with BRAF\^V600 mutation-positive malignancies. The study has two periods: Period A and Period B. During Period A, participants will receive vemurafenib BID orally from Day 1 to Day 20 and during Period B, participants will receive single IV infusion of 14C-labeled vemurafenib along with vemurafenib BID oral dose.

Who can participate

Age range18 Years

SexALL

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AI-rewrites the medical criteria so a patient or caregiver can understand them. Always confirm with the trial site.

Inclusion Criteria: * Participants with either unresectable or metastatic melanoma positive for the BRAF\^V600 mutation or other malignant tumor type that harbors a V600-activating mutation of BRAF, and for whom vemurafenib is an accepted standard of care or where there is no other generally accepted standard of care * Eastern Cooperative Oncology Group (ECOG) performance status 0 to 2 * Life expectancy greater than or equal to (\>/=) 12 weeks * Full recovery from the effects of any major surgery or significant traumatic injury within 14 days from the first dose of study drug * Adequate hematologic and end organ function as defined by laboratory results obtained within 2 weeks prior to administration of study drug on Day 1 * Female participants of childbearing potential and male participants with partners of childbearing potential must agree to use two effective methods of contraception during the study and at least 6 months after completion of the study drug * Negative serum pregnancy test results within 7 days prior to Day 1 in women of childbearing potential * Absence of any psychological, familial, or sociological condition, or geographical constraints that could potentially hamper compliance with the study protocol and follow-up schedule Exclusion Criteria: * Prior anti-cancer therapy before the administration of study drug on Day 1 * Invasive malignancy other than BRAF mutant melanoma or other qualifying malignant tumor with BRAF\^V600 mutation within the past 5 year…

What they're measuring

Area Under the Concentration-Time Curve (AUC) of 14C-Labeled Vemurafenib From Time 0 to Last Measurable Concentration Timepoint (AUC0-last)

Timeframe: Day 21: Predose (Hour 0); end of infusion (infusion duration: 15 minutes); 5, 15 and 30 minutes post-infusion; 1, 2, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 168 hours post-infusion of 14C-labeled vemurafenib

AUC of 14C-Labeled Vemurafenib From Time 0 to Infinity (AUC0-inf)

AUC of Unlabeled Vemurafenib During the Dosing Interval (AUCtau)

Timeframe: Predose (0 hour) on Days 18, 19, 20; Day 21: pre-dose (0 hour), 15 minutes after oral dose (at the end of IV infusion), at 30 and 45 minutes, and 1.15, 2.25, 3.25, 4.25, 6.25, 8.25, and 12 hours following oral administration of unlabeled vemurafenib

Maximum Observed Plasma Concentration (Cmax) of 14C-Labeled Vemurafenib

Terminal Half-Life (t1/2) of 14C-Labeled Vemurafenib

Trial details

NCT IDNCT02441465

SponsorHoffmann-La Roche

Sponsor typeINDUSTRY

Study typeINTERVENTIONAL

Primary completion2016-08-18

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