Table 1.

DNA damage response–modulating drugs in clinical development, grouped by repair pathway targeted

AgentCompanyAdministrationSingle and/or Combination TherapyDisease indicationsClinical status
Direct repair (MGMT)
O6benzylguanineCombination BCNUGBMPhase II complete
LomeguatribKuDosOralCombination with TMZMelanomaPhase II complete
Single-strand break repair (PARP inhibitors, PARPi)
PF0367338 (AG014699)PfizerIVCombination ++ single agentSolid tumors, melanomaPhase I and II complete and others ongoing
Olaparib (AZD2281)AztraZeneca (KuDos)OralCombination ++ single agentBRCA defective, solid tumors variousPhase I and II studies completed and ongoing
Veliparib (ABT888)AbbottOralCombination ++Various solid tumorsPhase I and II studies completed and ongoing
Iniparib (SAR240550, BSI 201)Sanofi Aventis (Bipar)IVCombinationTriple negative breastPhase III complete
MK4827MerckOralSingle agentSolid, BRCA ovarianPhase I ongoing
CEP-9722CephalonOralCombination with TMZSolid tumorsPhase I ongoing
E7016 (GPI 21016)Eisai (MGI Pharma)OralCombination with TMZSolid tumorsPhase I ongoing
LT673BiomarinOralSolid tumorsPhase I planned
Single-strand break repair (APE1 inhibitors APE1i)
TRC102TraconOralCombination with pemetrexedSolid tumorsPhase I complete
MethoxyamineIVCombination with TMZSolid tumorsPhase I suspended
DSB repair (RAD51 inhibitor, RAD51i)
MP470SupergenOralSingle agentLymphoma and/or solid tumorsPhase I ? opened
DSB repair (ATM inhibitor, ATMi)
KU55933AstraZeneca (KuDos)???Preclinical
DSB repair (DNA PK inhibitor, DNA PKi)
NU7441AstraZeneca (KuDos)???Preclinical

NOTE. Data taken from ( compounds that are thought to be in late preclinical development are also included for completeness.

Abbreviations: IV, intravenous; TMZ, temozolomide; GBM, glioblastoma multiforme; BCNU, carmustine or bis-xhloronitrosourea; ? indicates clinical studies not yet initiated.