Pegdinetanib

Last updated
Pegdinetanib
Pegdinetanib non-peptide structure.svg
Clinical data
Trade names Angiocept
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
Formula C468H729N125O139S(un-PEGylated peptide)
Molar mass 10362.78 g·mol−1

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]

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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