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Phase 1 N=46 Treatment

A Study of Vemurafenib (Zelboraf) in Chinese Participants With BRAF V600 Mutation-Positive Unresectable or Metastatic Melanoma

Malignant Melanoma

Enrolled (actual)
46
Serious AEs
6.5%
Results posted
Jun 2016
Primary outcome: Primary: Area Under the Plasma Concentration-Time Curve (AUC) of RO5185426 From 0 to 8 Hours on Day 1 — 37.54 h*μg/mL

Study Design & Population

Study type
Interventional
Phase
Phase 1
Interventions
Vemurafenib (Drug)
Age
Adult, Older Adult · 18+ yrs
Sex
All
Sponsor
Hoffmann-La Roche
Primary completion
Oct 2013

Outcome Measures

OutcomeResultp-value
PRIMARY
Area Under the Plasma Concentration-Time Curve (AUC) of RO5185426 From 0 to 8 Hours on Day 1
37.54
PRIMARY
AUC of RO5185426 From 0 to 8 Hours on Day 21
501.28
PRIMARY
AUC of RO5185426 From 0 to 12 Hours on Day 1
57.51
PRIMARY
AUC of RO5185426 From 0 to 12 Hours on Day 21
720.31
PRIMARY
Maximum Plasma Concentration (Cmax) of RO5185426 on Day 1
6.93
PRIMARY
Cmax of RO5185426 Following Day 21 Dose
77.55
PRIMARY
Time of Maximum Plasma Concentration (Tmax) of RO5185426 on Day 1
4.97
PRIMARY
Tmax of RO5185426 Following Day 21 Dose
1.00
PRIMARY
AUC From 0 to 168 Hours of RO5185426 Following Day 21 Dose
4328.15
PRIMARY
Elimination Half-Life (t1/2) of RO5185426 Following Day 21 Dose
35.56
PRIMARY
Trough Plasma Concentration (Ctrough) of RO5185426 on Day 15
63.000
PRIMARY
Ctrough of RO5185426 on Day 19
65.595
PRIMARY
Ctrough of RO5185426 on Day 21
72.583
PRIMARY
Accumulation Ratio of RO5185426 AUC From 0 to 8 Hours Between Day 21 and Day 1
17.9
PRIMARY
Terminal Elimination Rate Constant (Kel) of RO5185426 on Day 21
0.02
SECONDARY
Percentage of Participants With a Best Overall Response of Complete Response (CR) or Partial Response (PR) According to Response Evaluation Criteria in Solid Tumors (RECIST) Version 1.1
52.2
SECONDARY
Percentage of Participants With Disease Progression or Death Among Participants With a Previous Assessment of CR or PR According to RECIST Version 1.1
54.2
SECONDARY
Duration of Response According to RECIST Version 1.1
9.13
SECONDARY
Percentage of Participants With Death or Disease Progression According to RECIST Version 1.1
69.6
SECONDARY
Progression-Free Survival (PFS)
8.25
SECONDARY
Percentage of Participants Who Died
80.4
SECONDARY
Overall Survival (OS)
18.7

Summary

This open-label, multicenter study will evaluate the pharmacokinetics, safety and efficacy of vemurafenib in Chinese participants with BRAF V600 mutation-positive unresectable or metastatic melanoma. Participants will receive vemurafenib 960 milligrams (mg) orally twice daily until disease progression or unacceptable toxicity occurs.

Eligibility Criteria

Inclusion Criteria

  • Chinese male or female participants, greater than or equal to (≥) 18 years of age
  • Histologically confirmed metastatic melanoma (surgically unresectable Stage IIIC or Stage IV, American Joint Committee on Cancer)
  • Treatment-naïve or having received prior systemic treatments for metastatic melanoma
  • Positive BRAF V600 mutation result determined by a designated laboratory using the Cobas 4800 BRAF V600 Mutation Test
  • Measurable disease by Response Evaluation Criteria in Solid Tumors (RECIST) v1.1
  • Previous allowed chemotherapy, immunotherapy, or radiation therapy must have been completed at least 2 weeks prior to study drug administration, and all associated toxicity must be resolved (to less than or equal to [≤] Grade 1 or baseline)
  • Recovery from effects of any major surgery (excluding tumor biopsy at baseline) or significant traumatic injury at least 14 days before the first dose of study treatment
  • Adequate hematologic, renal, and liver function as defined by protocol
  • Fertile men and women must use an effective method of contraception during treatment and for ≥6 months after completion of treatment as directed by their physician (in accordance with local requirements).
  • Eastern Cooperative Oncology Group (ECOG) performance status of 0 or 1
  • Life expectancy greater than (>) 3 months
  • Able to swallow pills

Exclusion Criteria

  • Active central nervous system (CNS) lesions (radiographically unstable/symptomatic lesions), except participants treated with stereotactic therapy or surgery who remain without evidence of disease progression in brain for ≥3 months and have been off corticosteroid and anticonvulsant therapy for ≥3 weeks
  • History of or known spinal cord compression or carcinomatous meningitis
  • Anticipated or ongoing administration of anti-cancer therapies other than those administered in this study
  • Active squamous cell carcinoma (SCC) that has not been excised or has not yet adequately healed post excision
  • Pregnant or lactating women
  • Refractory nausea and vomiting, malabsorption, external biliary shunt, or significant small bowel resection that would preclude adequate vemurafenib absorption
  • Any of the following within the 6 months prior to study drug administration: myocardial infarction, severe/unstable angina, coronary/peripheral artery bypass graft, symptomatic congestive heart failure, serious cardiac arrhythmia requiring medication, uncontrolled hypertension, cerebrovascular accident or transient ischemic attack, or symptomatic pulmonary embolism
  • Known clinically significant active infection
  • History of allogeneic bone marrow transplantation or organ transplantation
  • Previous malignancy within the past 5 years other than adequately treated basal cell carcinoma or SCC of the skin, melanoma in-situ, and carcinoma in-situ of the cervix and/or curatively treated cancer from which the participant is currently disease-free, or any malignancy from which the participant has been continuously disease-free for at least 5 years
  • Previous treatment with a BRAF inhibitor (sorafenib allowed) or MEK inhibitor
  • Participants who have had one or more doses of vemurafenib in a previous clinical trial
  • Known human immunodeficiency virus (HIV) positivity or acquired immune deficiency syndrome (AIDS)-related illness, or hepatitis B virus or hepatitis C virus (HCV) carriers (hepatitis B surface antigen-positive, HCV antibody-positive)
  • Received any investigational treatment within 4 weeks of study drug start
View full record on ClinicalTrials.gov →

Data sourced from ClinicalTrials.gov (NCT01910181). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication.

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