A phase I trial of the Hedgehog inhibitor, sonidegib (LDE225), in combination with etoposide and cisplatin for the initial treatment of extensive stage small cell lung cancer

Lung Cancer. 2016 Sep:99:23-30. doi: 10.1016/j.lungcan.2016.04.014. Epub 2016 Apr 26.

Abstract

Objectives: The Hedgehog pathway has been implicated in small cell lung cancer (SCLC) tumor initiation and progression. Pharmacologic blockade of the key Hedgehog regulator, Smoothened, may inhibit these processes. We performed a phase I study to determine the maximum tolerated dose (MTD) of sonidegib (LDE225), a selective, oral Smoothened antagonist, in combination with etoposide/cisplatin in newly diagnosed patients with extensive stage SCLC.

Materials and methods: Patients received 4-6 21-day cycles of etoposide/cisplatin with daily sonidegib. Patients with response or stable disease were continued on sonidegib until disease progression or unacceptable toxicity. Two dose levels of sonidegib were planned: 400mg and 800mg daily, with 200mg daily de-escalation if necessary. Next generation sequencing was performed on available specimens. Circulating tumor cells (CTCs) were quantified at baseline and with disease evaluation.

Results: Fifteen patients were enrolled. 800mg was established as the recommended phase II dose of sonidegib in combination with etoposide/cisplatin. Grade 3 or greater toxicities included: anemia (n=5), neutropenia (n=8), CPK elevation (n=2), fatigue (n=2), and nausea (n=2). Toxicity led to removal of one patient from study. Partial responses were confirmed in 79% (11/14; 95% CI: 49-95%). One patient with SOX2 amplification remains progression-free on maintenance sonidegib after 27 months. CTC count, at baseline, was associated with the presence of liver metastases and after 1 cycle of therapy, with overall survival.

Conclusions: Sonidegib 800mg daily was the MTD when administered with EP. Further genomic characterization of exceptional responders may reveal clinically relevant predictive biomarkers that could tailor use in patients most likely to benefit.

Keywords: Circulating tumor cells; Hedgehog inhibitor; Hedgehog pathway; LDE225; SOX2 amplification; Small cell lung cancer.

Publication types

  • Clinical Trial, Phase I

MeSH terms

  • Antineoplastic Combined Chemotherapy Protocols / adverse effects
  • Antineoplastic Combined Chemotherapy Protocols / therapeutic use*
  • Biphenyl Compounds / administration & dosage
  • Biphenyl Compounds / pharmacokinetics
  • Cisplatin / administration & dosage
  • Cisplatin / pharmacokinetics
  • Etoposide / administration & dosage
  • Etoposide / pharmacokinetics
  • Female
  • Hedgehog Proteins / antagonists & inhibitors
  • Humans
  • Lung Neoplasms / drug therapy*
  • Lung Neoplasms / mortality
  • Lung Neoplasms / pathology*
  • Male
  • Maximum Tolerated Dose
  • Neoplasm Staging
  • Neoplastic Cells, Circulating
  • Pyridines / administration & dosage
  • Pyridines / pharmacokinetics
  • Small Cell Lung Carcinoma / drug therapy*
  • Small Cell Lung Carcinoma / mortality
  • Small Cell Lung Carcinoma / pathology*
  • Treatment Outcome

Substances

  • Biphenyl Compounds
  • Hedgehog Proteins
  • Pyridines
  • sonidegib
  • Etoposide
  • Cisplatin