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2007 Antiretrovirals in Development Pipeline

By Rob Camp

March 23, 2007

NRTIs, NNRTIs and Protease Inhibitors
Phase of Development NRTI NNRTI PI
Preclinical BPH-218, bis-phosphonate NRTI, U Pittsburgh
C-8 substituent,
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


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.

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,

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,

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


* 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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