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A Study on the Effect of Vemurafenib on the Pharmacokinetics of a Single Dose of Tizanidine in Patients With BRAFV600 Mutation-Positive Metastatic Malignancies

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Roche

Status and phase

Completed
Phase 1

Conditions

Malignant Melanoma, Neoplasms

Treatments

Drug: Tizanidine
Drug: Vemurafenib

Study type

Interventional

Funder types

Industry

Identifiers

NCT01844674
GO28396
2012-003705-94 (EudraCT Number)

Details and patient eligibility

About

This open-label, multicenter, 3-period, fixed-sequence study will evaluate the effect of multiple oral doses of vemurafenib on the pharmacokinetics of a single oral dose of tizanidine in participants with BRAFV600 mutation-positive metastatic malignancies. Participants will receive a single oral dose of tizanidine on Day 1, vemurafenib orally twice daily on Days 2 to 21, and tizanidine and vemurafenib on Day 22. Eligible participants will have the option to continue treatment with vemurafenib as part of an extension study (NCT01739764).

Enrollment

18 patients

Sex

All

Ages

18 to 70 years old

Volunteers

No Healthy Volunteers

Inclusion criteria

  • Adults 18 to 70 years of age, inclusive
  • Unresectable Stage IIIc or IV metastatic melanoma positive for the BRAFV600 mutation or other malignant tumor type which harbors a V600 activating mutation of BRAF, as determined by Cobas 4800 BRAFV600 Mutation Test or a DNA sequencing method
  • Eastern Cooperative Oncology Group (ECOG) performance status 0 to 2
  • Life expectancy greater than or equal to (>/=) 12 weeks
  • Participant has not consumed tobacco or nicotine-containing products for 42 days prior to first dose of study drug, and must agree to refrain from such products while on study
  • Adequate hematologic, renal and liver function

Exclusion criteria

  • Prior treatment with vemurafenib or other BRAF inhibitor within 42 days of Day 1
  • History of or current clinically significant cardiac or pulmonary dysfunction, including current uncontrolled Grade >/= 2 hypertension or unstable angina
  • Current dyspnea at rest due to complications of advanced malignancy or any requirement for supplemental oxygen
  • Active central nervous system lesions (participants with radiographically unstable, symptomatic lesions)
  • Participants with CYP1A2 gene mutation (-3113G->A), either in one or two alleles
  • Allergy or hypersensitivity to vemurafenib or tizanidine formulations
  • Current severe uncontrolled systemic disease
  • Inability or unwillingness to swallow pills
  • History of malabsorption or other condition that would interfere with enteral absorption of study treatment
  • History of clinically significant liver disease (including cirrhosis), current alcohol abuse, or human immunodeficiency (HIV) infection requiring antiretroviral treatment, acquired immune deficiency syndrome (AIDS)-related illness, or active hepatitis B or C
  • Pregnant or breastfeeding women

Trial design

Primary purpose

Other

Allocation

N/A

Interventional model

Single Group Assignment

Masking

None (Open label)

18 participants in 1 patient group

Pharmacokinetic Population
Experimental group
Description:
All participants will receive a 3-period treatment including single-dose tizanidine on Day 1, twice-daily vemurafenib on Days 2 to 21, and both agents together on Day 22.
Treatment:
Drug: Tizanidine
Drug: Vemurafenib

Trial contacts and locations

12

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Data sourced from clinicaltrials.gov

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