TABLE 1 | Ongoing clinical trials of small-molecule inhibitors of the DNA damage response and related signalling pathways

From the following article:

DNA repair pathways as targets for cancer therapy

Thomas Helleday, Eva Petermann, Cecilia Lundin, Ben Hodgson & Ricky A. Sharma

Nature Reviews Cancer 8, 193-204 (March 2008)

doi:10.1038/nrc2342

Agent (company)Target molecule or pathwayMonotherapy or combination therapy agent(s)Phase of clinical trial planned, ongoing or recently completedReference
AZD-2281 (Astra Zeneca)PARPGemcitabine
Carboplatin
Topotecan
Monotherapy
Phase I
Phase I
Phase I
Phase II
http://www.astrazenecaclinicaltrials.com/article/525925.aspx
AG014699 (Pfizer)PARPTemozolomide antibody
Temozolomide
Phase I
Phase II
http://www.eddn.org/clinicalTr_caResUK.html
INO-1001 (Inotek)PARPTemozolomidePhase Ihttp://www.inotekcorp.com/content/ino-1001.asp
BSI-201 (Bipar Sciences)PARPMonotherapy
Gemcitabine–carboplatin
Phase I
Phase II
http://www.biparsciences.com/BSI201.html
ABT-888 (Abbott Laboratories)PARPTemozolomidePhase INCT00526617
TRC-102 (Tracon Pharma)BERTemozolomide
Pemetrexed
Phase I
Phase I planned
http://www.traconpharma.com/content/pipeline_overview.html
Lomeguatrib (Astra Zeneca)MGMTIrinotecan
Temozolomide
Phase I
Phase II
http://www.astrazenecaclinicaltrials.com/article/525925.aspx
O6-BenzylguanineMGMTTemozolomidePhase IIhttp://clinicalstudies.info.nih.gov/cgi/detail.cgi?A_2006-C-0089.html
Decitabine (MGI Pharma121)Hypermethylation of mismatch repair genesEpirubicin, cisplatin, 5-fluorouracil
Carboplatin
Phase I
Phase II
http://pfsearch.ukcrn.org.uk/StudyDetail.aspx?TopicID=&StudyID=2192
XL844 (Exilixis122)CHK1, CHK2GemcitabinePhase I plannedhttp://www.exelixis.com/pipeline_xl844.shtml
The recent or current stage of development of clinical trials is indicated for individual compounds, which are grouped by molecular target. BER, base excision repair; CHK, checkpoint kinase; MGMT, O-6-methylguanine methyltransferase; PARP, poly(ADP-ribose) polymerase.

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