2005 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 |
| Dinucleoside polyphosphates, NRTI "potentiators" U Miami |
Tricyclic NNRTI, BMS |
PPL-100, Procyon BioPharma
|
Betulinic Acid Derivatives (BAD), U North Carolina |
Carbazole derivative, NIID, Japan |
Chloroquine, Catholic U, Rome |
CNI-1493, Rev inhibitor, Heinrich Pette Institute, Germany | |
| siRNA molecule, CombiMatrix |
SMP-717, Advanced Life Sciences |
UIC02031, Kumamoto U, Japan |
KRH-2731, X4 antagonist, Kureha |
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 |
Resistant-repellant PI, Sequoia Pharmaceuticals | PRO-140, monoclonal antibody (MAb), Progenics |
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 |
GBV-C, virus that increases chemokines including RANTES (CCR5 blocker), U Iowa
|
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 | 15K & 15D, co-receptor docking inhibitors, NCI | Mycelium integrasone, Fungal polyketide, Merck | RSC-1838, GSK/Shionogi | ||
| 4-Ed4T, Kagoshima U |
BILR 355 BS/r, BI |
Cycloamides, Univ Illinois | RC-112 & Retrocyclin-1, θ-Defensins, DASTLR
|
Indolicidin, NIH | siRNA molecule, Nef inhibitor, CombiMatrix | ||
| Thiovir, foscarnet analog, Adventrx |
Thiazol derivatives, Inst for Virus Research,
Japan
|
D5, artificial gp41 MAb, Merck
|
Beta-diketo acids, U Parma/Sassari, Italy | Resveretol, Egr1 gene activator, NCI | |||
| Herpesvirus saimiri, transcription and post-transcription
antiviral, Temple U |
Quinolones, Wellcome Trust |
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 | 004, CCR5 mAB, Human Genome Sciences
|
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 | BL-1050, regulatory protein inhibitor, BioLine Rx
|
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| Branched 3 primers, U Illinois | UMIST, Genetic Innovation Network |
Theophylline, caffeine-related methylxanthine, Thomas Jefferson U |
CNI-1493, Rev inhibitor, Cytokine Pharmasciences
|
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| 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
|
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| AMD-887, CCR5 antagonist, Anormed
|
(12) rev inhibitors, NIH
|
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| RANTES analogs, CCR5 down-modulator, U Geneva
|
Glycodendrimers, lipid raft carbohydates, Penn State
|
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| SP10, Entry Inhibitor, Samaritan Pharma | siRNA constructs, rev/tat inhibitors, Beckman
Institute |
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| gp120-gp41 disulfide bond,
Amsterdam MC, Cornell U, U Illinois Chicago |
HRG214, caprine IgG, Virionyx, New Zealand |
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| Pyrrolidine CCR5 receptor antagonists, Merck | |||||||
| NSC 13778, gp120 blockers, SAIC-NCI | |||||||
| sifuvirtide, fusion inhibitor, Fusogen |
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| gp41 inhibitors, New York Blood Center |
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| Phase I | KP-1461, mutagenic deoxyribo-nucleoside, Koronis
|
BMS-378806, gp120 blocker, BMS |
JTK-303, Gilead | αHGA, Tripep | Mifepristone, glucocorticoid antagonist, U Pittsburgh |
||
| 695634, GSK
|
AK602, CCR5 inhibitor, Kumamoto Unioversity | ||||||
| DOT, dioxolane thymidine, U Georgia
|
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| Phase I/II or Phase IB | Racivir (PSI 5004), Pharmasset/Incyte |
TMC-278, Diarylpyrimidine (DAPY), Tibotec
|
640385, GSK |
873140, CCR5 antagonist, GSK/ONO
|
PA-457, Budding inhibitor, Vitex/Panacos
|
||
| AVX754, Avexa Ltd
|
BMS-043, BMS |
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| Phase II | Elvucitabine (ACH-126), Achillion
|
Calanolide A, Advanced Life Sciences |
PRO-542, attachment inhibitor, Progenics |
||||
| Amdoxovir (DAPD), RFS Pharm
|
TMC-125 (etravirine), Tibotec/J&J |
UK-427 (Maraviroc), CCR5 antagonist, Pfizer
|
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| Reverset (D-D4FC), Pharmasset/Incyte
|
AMD-070, CXCR4 antagonist, Anormed
|
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| Vicriviroc (SCH 417, SCH D), CCR5 antagonist, Schering Plough
|
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| TNX-355, Anti-CD4 MAb, Tanox/Biogen
|
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| Phase III | TMC-114/r, Tibotec/J&J |
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 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 materialsRecent news from the XIIth Conference on Retroviruses and Opportunistic Infections, Boston, 22-25 February, 2005 |
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