Su-6668. SUGEN

Curr Opin Investig Drugs. 2001 Aug;2(8):1142-8.


SUGEN is developing SU-6668, a tyrosine kinase inhibitor that inhibits three distinct growth factor receptor targets, for the potential treatment of cancer [304530]. The compound is in phase I trials in the UK and US [321260], [374505]. A report in January 2001 stated that phase I/II trials for hematological and solid tumors were expected to commence shortly thereafter [395657]. In May 2001, phase I data from a dose-escalation study conducted at UCLA were presented at the 37th ASCO meeting in San Francisco, CA. By that time, 74 patients had been enrolled in this study which aimed to determine the toxicities of SU-6668 when delivered to fed and fasting patients. SU-6668 was administered orally either once or twice-daily at doses of 100 to 2400 mg/m2 to patients diagnosed as having advanced malignancies. Accrual in phase I is continuing to define the toxicities of doses > 200 mg/m2 twice-daily [409984], [411418]. In December 1998, SUGEN filed an IND with the FDA for the clinical testing of this compound with oral and iv formulations [310237]. In November 1998, SUGEN entered into a collaboration with the Cancer Research Campaign (CRC) to conduct a phase I trial of SU-6668 at the Royal Marsden Hospital, UK using an iv formulation [304530]. After the first six patients had been treated, the trial was halted owing to problems with the iv formulation. Some toxicities, including nausea, vomiting, fatigue and tumor pain were observed [413538]. No licensing agreement as involved between the CRC and SUGEN for this trial [408572].

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / adverse effects
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / metabolism
  • Antineoplastic Agents / pharmacology*
  • Antineoplastic Agents / therapeutic use
  • Antineoplastic Agents / toxicity
  • Enzyme Inhibitors / pharmacology
  • Humans
  • Indoles / adverse effects
  • Indoles / chemical synthesis
  • Indoles / metabolism
  • Indoles / pharmacology*
  • Indoles / therapeutic use
  • Indoles / toxicity
  • Neoplasms / drug therapy
  • Protein-Tyrosine Kinases / antagonists & inhibitors
  • Pyrroles / adverse effects
  • Pyrroles / chemical synthesis
  • Pyrroles / metabolism
  • Pyrroles / pharmacology*
  • Pyrroles / therapeutic use
  • Pyrroles / toxicity
  • Structure-Activity Relationship


  • Antineoplastic Agents
  • Enzyme Inhibitors
  • Indoles
  • Pyrroles
  • orantinib
  • Protein-Tyrosine Kinases