Phase 1 trial of tivantinib in combination with sorafenib in adult patients with advanced solid tumors

Invest New Drugs. 2015 Feb;33(1):159-68. doi: 10.1007/s10637-014-0167-5. Epub 2014 Oct 8.

Abstract

Purpose: This phase I study evaluated the safety, tolerability, maximum tolerated dose (MTD), and recommended phase II dose (RP2D) of tivantinib combined with sorafenib in patients with advanced solid tumors.

Materials and methods: A standard 3 + 3 dose escalation design was used. At the RP2D, expansion cohorts in 5 tumor types could be enrolled. Pharmacogenetic and pharmacodynamic analysis were performed.

Results: Eighty-seven patients received the study treatment. The combination had no unexpected toxicities. The most common treatment-related adverse events (AE) were rash (40 %), diarrhea (38 %), and anorexia (33 %). The RP2D was tivantinib 360 mg BID and sorafenib 400 mg BID for all cancer histologies, except in hepatocellular carcinoma (HCC) patients tivantinib was 240 mg BID plus sorafenib 400 mg BID. The overall response rate was 12 % in all patients, 26 % in melanoma, 15 % in renal cell carcinoma (RCC), 10 % in HCC, and 0 % in other patients. Disease control rate (CR, PR and SD ≥8 weeks) was 58 % in all patients, 90 % in RCC, 65 % in HCC, 63 % in melanoma, 40 % in breast cancer, and 8 % in NSCLC patients.

Conclusions: The combination treatment could be administered at full standard single-agent doses in all patients except those with HCC, where tivantinib was lowered to 240 mg BID. Preliminary evidence of anticancer activity was observed in patients with RCC, HCC, and melanoma, including patients refractory to sorafenib and/or other anti-VEGF pathway therapies. The combination treatment has therapeutic potential in treating a variety of solid tumors.

Publication types

  • Clinical Trial, Phase I
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Aged
  • Aged, 80 and over
  • Antineoplastic Combined Chemotherapy Protocols / adverse effects
  • Antineoplastic Combined Chemotherapy Protocols / pharmacokinetics
  • Antineoplastic Combined Chemotherapy Protocols / pharmacology
  • Antineoplastic Combined Chemotherapy Protocols / therapeutic use*
  • Cytochrome P-450 CYP2C19 / genetics
  • Female
  • Humans
  • Male
  • Maximum Tolerated Dose
  • Middle Aged
  • Neoplasms / drug therapy*
  • Neoplasms / genetics
  • Neoplasms / metabolism
  • Niacinamide / administration & dosage
  • Niacinamide / adverse effects
  • Niacinamide / analogs & derivatives
  • Niacinamide / pharmacokinetics
  • Niacinamide / pharmacology
  • Phenylurea Compounds / administration & dosage
  • Phenylurea Compounds / adverse effects
  • Phenylurea Compounds / pharmacokinetics
  • Phenylurea Compounds / pharmacology
  • Polymorphism, Genetic
  • Proto-Oncogene Proteins c-met / metabolism
  • Pyrrolidinones / administration & dosage
  • Pyrrolidinones / adverse effects
  • Pyrrolidinones / pharmacokinetics
  • Pyrrolidinones / pharmacology
  • Quinolines / administration & dosage
  • Quinolines / adverse effects
  • Quinolines / pharmacokinetics
  • Quinolines / pharmacology
  • Sorafenib
  • Treatment Outcome
  • Young Adult

Substances

  • ARQ 197
  • Phenylurea Compounds
  • Pyrrolidinones
  • Quinolines
  • Niacinamide
  • Sorafenib
  • CYP2C19 protein, human
  • Cytochrome P-450 CYP2C19
  • MET protein, human
  • Proto-Oncogene Proteins c-met