Inhibitor timidilatne sintaze

Inhibitori timidilatne sintaze su hemijski agensi koji inhibiraju enzim timidilatna sintaza, te mogu da nađu primenu u antikancernoj hemoterapiji.[1] Pet agenasa je bilo u kliničkim israživanjima 2002: raltitreksed, pemetreksed, nolatreksed, ZD9331, i GS7904L.[2]

Primeri lekova ove klase su:

  • Raltitreksed, koristi se za kolorektalni kancer od 1998
  • Fluorouracil, koristi se za kolorektalni kancer[3]
  • BGC 945[4]
  • OSI-7904L[5]

Reference

  1. Jackman, A.L.; Calvert, A.H. (1995). „Folate-based thymidylate synthase inhibitors as anticancer drugs”. Annals of Oncology 6 (9): 871–881. 
  2. „Thymidylate synthase inhibitors as anticancer agents: from bench to bedside”. Pristupljeno 2009-01-28. 
  3. Papamichael, D. (1999). „The use of thymidylate synthase inhibitors in the treatment of advanced colorectal cancer: current status”. Oncologist 4 (6): 478–87. PMID 10631692. [mrtav link]
  4. Gibbs, David D., et al (2005). „BGC 945, a novel tumor-selective thymidylate synthase inhibitor targeted to α-folate receptor-overexpressing tumors”. Cancer Research 65 (24): 11721–11728. DOI:10.1158/0008-5472.CAN-05-2034. 
  5. Ricart AD, Berlin JD, Papadopoulos KP, et al. (December 2008). „Phase I, pharmacokinetic and biological correlative study of OSI-7904L, a novel liposomal thymidylate synthase inhibitor, and cisplatin in patients with solid tumors”. Clin. Cancer Res. 14 (23): 7947–55. DOI:10.1158/1078-0432.CCR-08-0864. PMID 19047127. 
  • p
  • r
  • u
Intracelularni hemoterapijski lekovi/Antineoplastični lekovi (L01)
SP/MI
(M faza)
Blokiranje formiranja microtubule
Blokiranje rasformiranja microtubule
Inhibitori
DNK replikacije
DNA prekursori/
antimetaboliti
(S faza)
II+Interkalacija
Interkalacija
Fotosensitizeri/PDTDrugi
FI (Tipifarnib)  • CDK inhibitori (Alvocidib, Seliciklib) • PrI (Bortezomib) • PhI (Anagrelid) • IMPDI (Tiazofurin) • LI (Masoprokol) • PARP inhibitor (Olaparib) • HDAC (Vorinostat, Romidepsin)
Receptorski antagonisti
ERA (Atrasentan) • retinoid X receptor (Beksaroten) • seks steroid (Testolakton)
Drugi/negrupisani

M: NEO

tmsp, onco, mrkr

tumr, epon, para

drug (L1i/1e)