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Table 1 PARP inhibitors under clinical investigation in malignant disease

From: Poly(ADP-ribose) polymerase inhibition: a new direction for BRCAand triple-negative breast cancer?

Agent (year entered clinical research)

Manufacturer

Single/combination therapy

Oral/intravenous

Clinical indication(s)

Status

AG014699, PF0367338 (2003)

Pfizer (New York, NY, USA)

Single agent; multiple combinations

Intravenous and oral

Solid tumours; melanoma; BRCA germline

Phase I and II melanoma studies complete. Phase II BRCA studies open

KU59436, AZD2281, olaparib (2005)

AstraZeneca/KuDOS (London, UK)

Single agent; multiple combinations

Oral

Various, including BRCA germline

Phase I complete. Numerous phase II studies ongoing

ABT-888, veliparib (2006)

Abbott Laboratories (North Chicago, IL, USA)

Multiple combinations

Oral

Solid tumours; melanoma; lymphoid malignancies

Phase 0/I completed in some indications Numerous phase II studies ongoing

BSI-201, SAR 240550 iniparib (2006)

BiPar (South San Francisco, CA, USA; Sanofi Aventis)

Combination with gemcitabine and carboplatin; temozolomide

Intravenous

TNBC; lung cancer; glioma

Phase II studies completed. Phase III study in TNBC recruiting. Phase II study in lung near completion

INO-1001 (2005/2006)

Inotek/Genentech (Lexington, MA, USA)

Single agent; combination with temozolomide

Intravenous

Melanoma; malignant glioma

Phase Ib in melanoma completed

MK4827 (2008)

Merck Sharp Dohme (Hoddesdon, UK)

Single agent; combination with chemotherapy

Oral

Solid tumours; BRCA- related ovarian cancer

Phase I ongoing

CEP-9722 (2009)

Cephalon (Frazer, PA, USA)

Single agent; combination with temozolomide

Oral

Solid tumours

Phase I ongoing

GPI 21016 (2010)

MGI Pharma (Bloomington, MN, USA)

Combination with temozolomide

Oral

Solid tumours

Phase I ongoing

E7016 (2010)

MGI Pharma (Bloomington, MN, USA), Eisai (Baltimore, MD, USA)

Combination with temozolomide

Oral

Solid tumours

Phase I ongoing

LT673 (2011)

Lead Therapeutics/Biomarin (Novato, CA, USA)

Single agent and combination planned

Oral

Solid tumours

Phase I planned

  1. PARP, poly(ADP-ribose) polymerase; TNBC, triple-negative breast cancer.