2007 Antiretrovirals in Development Pipeline

By Rob Camp
From Treatment Action Group

March 23, 2007

NRTIs, NNRTIs and Protease Inhibitors
Entry Inhibitors, Integrase Inhibitors, Maturation Inhibitors and Other Drugs

NRTIs, NNRTIs and Protease Inhibitors
Phase of Development	NRTI	NNRTI	PI
Preclinical	BPH-218, bis-phosphonate NRTI, U Pittsburgh	C-8 substituent, BI	AG-1859, Pfizer
	Dinucleoside polyphosphates, NRTI "potentiators" U Miami	GS9148 and GS9148 prodrug, Gilead	GRL-02031, Kumamoto U
	DOT-TP, Emory U	SMP-717, Advanced Life Sciences	UIC02031, Kumamoto U, Japan
	Compound X, nucleotide-competing indolopyridone, Tibotec	SMP-610, Advanced Life Sciences	SPI-256, Sequoia Pharm
	KMMP05, RNase H Inhibitor, NCI	S-DABO derivatives (HIV-1 and -2) and pyrimidinediones, Fudan U, China	Beta lactams, University of Debrecen, Hungary
	D-FDOC, Emory Univ.	Oligodeoxi-nucleotides, U Hospital, Zurich	A-681799, Abbott
	4-Ed4T, Kagoshima U	PBO-15c, pyrrolobenzoxazepinone, U Siena	D5, artificial gp41 MAb, Merck
	Thiovir, foscarnet analog, Adventrx	Thiazol derivatives, Inst for Virus Research, Japan
	Herpesvirus saimiri, transcription and post-transcription antiviral, Temple U	Methyl derivatives, U South Denmark
	Triol, diterpine RTI, Cruz Foundation, Brasil	MV026048 and MIV-170, Medivir
	Stampidine, Parker Hughes Institute	Phenylthiazoylamines, Yale U
	Branched 3 primers, U Illinois	HBY 097 and pyridinone derivatives, Rutgers U
	dTTP, U Rochester	AR806, Ardea BioSc
	E2-FdA, Kumamoto U
	DOT, dioxolane thymidine, U Georgia
	R12-2, thioaptamer, RNaseH domain blocker, U Texas
	Didox, Ribonucleotide reductase (RR) inhibitor, Molecules for Health
	Quinolones, Rega Institute
	TSAO-T derivatives, U Pittsburgh
	Thiostavudines, Showa U
	ARC, Howard U
Phase I	KP-1461, mutagenic deoxyribo-nucleoside, Koronis	70h, GSK	PPL-100, Merck
	Alovudine (fosalvudine tidoxil, FLT), Heidelberg Pharma
Phase Ib/II	Racivir (PSI 5004), Pharmasset	BILR 355/r, BS, Boehringer Ingelheim
	Apricitabine (AVX754), Shire	UK-435, 061, Pfizer
	Elvucitabine (ACH-126), Achillion
Phase II		Rilpivirine, TMC-278, Tibotec/J&J
Phase III		Etravirine (TMC125), Tibotec/J&&J
Notes: On hold or stopped. link to abstract/background material from CROI 2005. Advertisement link to abstract/background material from XIIIth Conference on Retroviruses and Opportunistic Infections, Denver, US, 5-8 February, 2006.

Entry Inhibitors, Integrase Inhibitors, Maturation Inhibitors and Other Drugs
Phase of Development	EI *	Integrase Inhibitors	Maturation Inhibitors**	Other
Preclinical	Benzothiepine & Benzazepine derivatives, 11f, and TAK-652, CCR5 antagonists, Takeda	L-second generation, Merck	enJS56A1, Escape Inhibitor, U Georgia	RWJ67567, p38 inhibitor, U Penn / J&J
	Betulinic Acid Derivatives (BAD), DSB/U North Carolina	Carbazole derivative, NIID, Japan	siRNA molecule, CombiMatrix	CNI-1493, Rev inhibitor, Heinrich Pette Institute, Germany
	Aprepitant, NK-1R antagonist	810871, GSK	Betulinic Acid Derivatives (BAD), U North Carolina	Trim5α capsid inhibitor, Dana Farber, NIAID
	GBV-C, virus that increases chemokines including RANTES (CCR5 blocker), U Iowa	Styrylquinoline derivatives, Bioalliance Pharma	ACH-CIP, capsid inhibitor, Achillion	CDK inhibitor, Gilead
	15K & 15D, co-receptor docking inhibitors, NCI	V-165, Rega Institute, Belgium	RPI-MN, ReceptoPharm	KU-55933, ATM kinase inhibitor, KuDOS Pharma
	RC-112 & Retrocyclin-1, θ-Defensins, DASTLR	Mycelium integrasone, Fungal polyketide, Merck	UK-201,844, Pfizer	RSC-1838, GSK/Shionogi
	Indolicidin, NIH	GS 9224, Gilead Sciences	siRNA molecule, Nef inhibitor, CombiMatrix	IM, CDK9 inhibitor, Inst of Human Virology
	Pyrrolidine CCR5 receptor antagonists, Merck	Beta-diketo acids, U Parma/Sassari, Italy	PA1050040-02, Panacos	Resveretol, Egr1 gene activator, NCI
	IC9564, Duke University	PL-2500, P-5-P derivative, Procyon		MDI-P, electrolyzed free radical, Medical Discoveries
	Zinc Finger Protein Nucleases, CCR5 inhibitors, Sangamo Biosciences	Monophores, Sunesis		Poly (acrylic) acid, Chinese Academy of Science
	MDX-010, anti-CTLA-4 antibody, Medarex	AVX-I, Avexa		α-v integrins, irsiCaixa Foundation/Merck
	UMIST, Genetic Innovation Network	Theophylline, caffeine-related methylxanthine, Thomas Jefferson U		CNI-1493, Rev inhibitor, Cytokine Pharmasciences
	NB-2 and NB-64, gp41 coiled coil blocker, Shibo & Kumar	ITI-367, Oxadiazol pre-integrase inhibitor, GWU		Curcumin (diferuloylmethane), Tat inhibitor, Jawaharlal Nehru Center, India
	AMD-887, CCR5 antagonist, Anormed	Triketoacid IIs, BMS		(12) rev inhibitors, NIH
	KD-247, CCR5 inhibitor, Kumamoto U			Glycodendrimers, lipid raft carbohydates, Penn State
	SP10, Samaritan			siRNA constructs, rev/tat inhibitors, Beckman Institute
	gp120-gp41 disulfide bond, Amsterdam MC, Cornell U, U Illinois Chicago			HRG214, caprine IgG, Virionyx, New Zealand
	NSC 13778, gp120 blockers, SAIC-NCI			RPI, nicotinic acetylcholine receptor blocker, NutraPharma
	sifuvirtide, fusion inhibitor, Fusogen			Oxadiazols, nuclear localization viral matrix blockers, International Therapeutics
	gp41 inhibitors, New York Blood Center			LEDGF-integrase competers, Catholic U Leuven, Belgium
	gp41 inhibitors, Locus Pharmaceuticals			SCY-635, Cyclophilin Inhibitor, Scynexis
	AMD-3451, CCR5/CXCR4 receptor antagonist, Anormed
	Monoclonal FAbs, gp41 blocker, NIH
	DP-178, fusion inhibitor, Weizmann Institute
	TR-999 and TR-1144, Trimeris/Roche
	KRH-3955 and KRH-3140, CXCR4 inhibitors, Kureha Corp
	Peptidic CCR5 inhibitor, Selexis
	Small molecule gp120 inhibitors, BMS
	INCB15050, CCR5 inhibitor, Incyte
	HGS101, CCR5 mAb, Human Genome Sciences
	ZFN, CCR5 disrupter, Sangamo BioSciences
	ROAb12, -13, -14, and -18, CCR5 mAbs, Roche
	Genistein, USU Bethesda
	TD0232, Avexa/TD
	Bifunctional (CD4 and CCR5) inhibitors, U Regensburg
Phase I	BMS-378806, gp120 blocker, BMS	GSK364735, GSK/Shionogi		BI-201, Tat inhibiting mAb, BioInvent
	TAK-652, Takeda
	004, mAB, Human Genome Sciences
	Suc-HSA, fusion inhibitor, Sanquin
	PF232798, CCR5 inhibitor, Pfizer
Phase I/II or Phase IB	PRO-140, MAb, Progenics			Valproic acid, [Depakote™, Abbott], ACTG
	INCB9471, CCR5 inhibitor, Incyte			Bevirimat (PA-457), Budding inhibitor, Panacos
	HGS004, CCR5 mAb, Human Genome Sciences
Phase II	Vicriviroc, CCR5 antagonist, Schering Plough	GS-9137, Gilead
	TNX-355, Anti-CD4 MAb, Tanox/Biogen
Phase III	Maraviroc, CCR5 antagonist, Pfizer	MK-0518, Merck
Notes: * entry inhibitors, including CCR5 and CXCR4 receptor binding antagonists and CD4 monoclonal antibodies directed at binding, fusion, and entry. ** includes the later replication stages of Assembly, Budding, and Maturation. On hold or stopped. link to abstract/background material from CROI 2005. link to abstract/background material from XIIIth Conference on Retroviruses and Opportunistic Infections, Denver, US, 5-8 February, 2006.

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This article was provided by Treatment Action Group.