Preclinical 2006 Antiretrovirals Pipeline 
Phase of Development |
NRTI |
NNRTI |
PI |
EI* |
Integrase Inhibitors |
Maturation Inhibitors** |
Other |
| Preclinical | BPH-218, bis-phosphonate NRTI, U Pittsburgh |
C-8 substituent, BI |
AG-1859, Pfizer |
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 |
GS9148 and GS9148 prodrug, Gilead 
|
pyridinone derivatives, Rutgers | GRL-02031, Kumamoto U |
Betulinic Acid Derivatives (BAD), DSB/U North Carolina |
Carbazole derivative, NIID, Japan |
siRNA molecule, CombiMatrix |
CNI-1493, Rev inhibitor, Heinrich Pette Institute, Germany | |
| DOT-TP, Emory U |
SMP-717, Advanced Life Sciences |
UIC02031, Kumamoto U, Japan |
Aprepitant, NK-1R antagonist |
810871, GSK | Betulinic Acid Derivatives (BAD), U North Carolina | Trim5α capsid inhibitor, Dana Farber, NIAID |
|
| Compound X, nucleotide-competing RTI, Tibotec
|
SMP-610, Advanced Life Sciences |
SPI-256, Sequoia Pharm |
GBV-C, virus that increases chemokines including RANTES (CCR5 blocker), U Iowa |
Styrylquinoline derivatives, Bioalliance Pharma
|
ACH-CIP, capsid inhibitor, Achillion |
CDK inhibitor, Gilead |
|
| KMMP05, RNase H Inhibitor, NCI |
S-DABO derivatives (HIV-1 and -2), Fudan U, China | Beta lactams, University of Debrecen, Hungary |
15K & 15D, co-receptor docking inhibitors, NCI | V-165, Rega Institute, Belgium |
RPI-MN, ReceptoPharm | KU-55933, ATM kinase inhibitor, KuDOS Pharma | |
| D-FDOC, Emory Univ.
|
Oligodeoxi-nucleotides, U Hospital, Zurich |
A-681799, Abbott | RC-112 & Retrocyclin-1, θ-Defensins, DASTLR |
Mycelium integrasone, Fungal polyketide, Merck | UK-201,844, Pfizer |
RSC-1838, GSK/Shionogi | |
| 4-Ed4T, Kagoshima U |
PBO-15c, pyrrolobenzoxazepinone, U Siena | D5, artificial gp41 MAb, Merck
|
Indolicidin, NIH | GS 9224, Gilead Sciences | siRNA molecule, Nef inhibitor, CombiMatrix | IM, CDK9 inhibitor, Inst of Human Virology |
|
| Thiovir, foscarnet analog, Adventrx |
Thiazol derivatives, Inst for Virus Research,
Japan
|
Pyrrolidine CCR5 receptor antagonists, Merck | Beta-diketo acids, U Parma/Sassari, Italy | Resveretol, Egr1 gene activator, NCI | |||
| Herpesvirus saimiri, transcription and post-transcription
antiviral, Temple U |
Methyl derivatives, U South Denmark | IC9564, Duke University |
PL-2500, P-5-P derivative, Procyon | MDI-P, electrolyzed free radical, Medical Discoveries | |||
| Triol, diterpine RTI, Cruz Foundation, Brasil |
MV026048 and MIV-170, Medivir | Zinc Finger Protein Nucleases, CCR5 inhibitors, Sangamo
Biosciences |
Monophores, Sunesis | Poly (acrylic) acid, Chinese Academy of Science | |||
| Stampidine, Parker Hughes Institute |
Phenylthiazoylamines, Yale U |
MDX-010, anti-CTLA-4 antibody, Medarex |
AVX-I, Avexa | α-v integrins, irsiCaixa Foundation/Merck |
|||
| Branched 3 primers, U Illinois | UMIST, Genetic Innovation Network |
Theophylline, caffeine-related methylxanthine, Thomas Jefferson U |
CNI-1493, Rev inhibitor, Cytokine Pharmasciences
|
||||
| dTTP, U Rochester | 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 |
||||
| E2-FdA, Kumamoto U |
AMD-887, CCR5 antagonist, Anormed |
Triketoacid IIs, BMS | (12) rev inhibitors, NIH |
||||
| DOT, dioxolane thymidine, U Georgia |
KD-247, CCR5 inhibitor, Kumamoto U |
Glycodendrimers, lipid raft carbohydates, Penn State |
|||||
| R12-2, thioaptamer, RNaseH domain blocker, U Texas | SP01A & SP10, entry inhibitors, Samaritan | siRNA constructs, rev/tat inhibitors, Beckman
Institute |
|||||
| Didox, Ribonucleotide reductase (RR) inhibitor, Molecules for Health | gp120-gp41 disulfide bond,
Amsterdam MC, Cornell U, U Illinois Chicago |
HRG214, caprine IgG, Virionyx, New Zealand |
|||||
| Dinucleoside polyphosphates, NRTI "potentiators" U Miami |
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 inibitors, BMS | |||||||
| INCB15050, CCR5 inhibitor, Incyte | |||||||
| HGS101, CCR5 mAb, Human Genome Sciences | |||||||
| ZFN, CCR5 disrupter, Sangamo BioSciences | |||||||
| ROAbs, CCR5 mAbs, Roche | |||||||
 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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