Pegdinetanib

Pegdinetanib (USAN; planned trade name Angiocept) is an investigational anti-cancer drug that acts as a selective antagonist of vascular endothelial growth factor receptor 2 (VEGFR-2), hindering vascularization of tumors. It is a genetically engineered peptide derivative based on the monobody technology, and is being developed by Adnexus.[1][2]

Pegdinetanib
Clinical data
Trade namesAngiocept
Other namesCT-322; BMS-844203
Routes of
administration		Intravenous
ATC code
  • None
Legal status
Legal status
  • Investigational
Identifiers
CAS Number
ChemSpider
  • none
UNII
KEGG
Chemical and physical data
FormulaC468H729N125O139S (un-PEGylated peptide)
Molar mass10362.78 g·mol−1

The drug has entered Phase II clinical trials investigating the treatment of glioblastoma in October 2007.[3][4] As of August 2012, it is also in Phase II trials for the treatment of non-small cell lung cancer[5] and colorectal cancer.[6]

Chemical structure

Pegdinetanib is a peptide consisting of 94 amino acids, with cysteine number 93 carrying a doubly methoxy-PEGylated maleimide derivative with a molecular mass of 40 kDa.[7]

References
  1. Tolcher AW, Sweeney CJ, Papadopoulos K, Patnaik A, Chiorean EG, Mita AC, et al. (January 2011). "Phase I and pharmacokinetic study of CT-322 (BMS-844203), a targeted Adnectin inhibitor of VEGFR-2 based on a domain of human fibronectin". Clinical Cancer Research. 17 (2): 363–71. doi:10.1158/1078-0432.CCR-10-1411. PMID 21224368.
  2. Mamluk R, Carvajal IM, Morse BA, Wong H, Abramowitz J, Aslanian S, et al. (2010). "Anti-tumor effect of CT-322 as an adnectin inhibitor of vascular endothelial growth factor receptor-2". mAbs. 2 (2): 199–208. doi:10.4161/mabs.2.2.11304. PMC 2840239. PMID 20190562.
  3. Clinical trial number NCT00562419 for "CT-322 in Treating Patients With Recurrent Glioblastoma Multiforme and Combination Therapy With Irinotecan" at ClinicalTrials.gov
  4. Bloom L, Calabro V (October 2009). "FN3: a new protein scaffold reaches the clinic". Drug Discovery Today. 14 (19–20): 949–55. doi:10.1016/j.drudis.2009.06.007. PMID 19576999.
  5. Clinical trial number NCT00850577 for "Ph II of a Novel Anti-angiogenic Agent in Combination With Chemotherapy for the Treatment of Non-Small Cell Lung Cancer" at ClinicalTrials.gov
  6. Clinical trial number NCT00851045 for "Ph II Trial of a Novel Anti-angiogenic Agent in Combination With Chemotherapy for the Second-line Treatment of Metastatic Colorectal Cancer" at ClinicalTrials.gov
  7. Statement On A Nonproprietary Name Adopted By The USAN Council: Pegdinetanib
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