REFERENCE MATERIALS on drugs in development and terminology

Notes from teleconferences and community meetings are listed according to each pharmaceutical company. There is a web page for each company. Follow these links: (Note: if there's no link, the company's page has not yet been set up.)

• Abbott Laboratories (ritonavir, lopinavir)
• Agouron Pharmaceuticals (delavirdine, capravirine, nelfinavir)
• Boehringer Ingelheim (nevirapine, tipranavir)
• Bristol-Myers Squibb (ddI, d4T, efavirenz, DPC083, atazanavir)
• Chiron Corporation (interleukin-2)
• Gilead Sciences (tenofovir)
• GlaxoSmithKline (AZT, 3TC, abacavir, Combivir, Trizivir, amprenavir, GW433908)
• Merck & Co. (indinavir, vaccines, integrase inhibitors)
• Roche (ddC, saquinavir, Fuzeon (T-20), T-1249 fusion inhibitors, pegylated interferon for Hep C)
• Serono (Human Growth Hormone)
• Schering-Plough (Schering C and D fusion inhibitors, pegylated interferon for Hep C)
• Tibotec-Virco (TMC120, TMC125, TMC114; genotypic and phenotypic testing; drug level testing)

Reference Materials:

A. General Resources
1. Drugs in Development, listed alphabetically with manufacturer. Source: Ben Cheng, Project Inform
2. Medscape's Quick Reference Guide to Antiretrovirals, last updated January 3, 2002. Includes antiretroviral summary tables, drug-drug combinations, antiretroviral resistance mutations, methadone/antiretroviral drug interactions, and TB medication/antiretroviral drug interactions
3. Medscape's Quick Reference Guide to New Antiretrovirals, an overview of antiretroviral agents currently under development, last updated January 3, 2002
4. New Mexico AIDS InfoNet fact sheet #401, Antiviral Drug Names. Includes HIV drugs approved or in clinical trials. Listed by class with generic name, trade name, other names, and manufacturer.

B. Glossaries

1. Acronyms
2. AmfAR Treatment Directory Glossary http://www.amfar.org/cgi-bin/iowa/bridge.html?table=AMFAR_GLOSSARY
3. CPCRA Glossary of Medical, Statistical, and Clinical Trials Terminology
   http://sdmc.cpcra.org/gloss.html
4. HIV/AIDS Medical Glossary from Gay Men's Health Crisis
   http://www.gmhc.org/living/treatment/glossary.html
5. San Francisco AIDS Foundation Glossary of HIV/AIDS Related Terms
   http://www.sfaf.org/treatment/glossary/

Note: in this version, compounds are in alphabetical order. In the original version they were grouped by class of compound. Updated June 10, 2002.

Compound	Class of Compound	Phase of Development	Pharmaceutical Company
AZT	nucleoside analogue RT inhibitor	Approved	GlaxoSmithKline
ddI	nucleoside analogue RT inhibitor	Approved	Bristol-Myers Squibb
ddC	nucleoside analogue RT inhibitor	Approved	Hoffman-La Roche
d4T	nucleoside analogue RT inhibitor	Approved	Bristol-Myers Squibb
3TC	nucleoside analogue RT inhibitor	Approved	GlaxoSmithKline
Abacavir	nucleoside analogue RT inhibitor	Approved	GlaxoSmithKline
Emtricitabine (FTC)	nucleoside analogue RT inhibitor	Phase III	Triangle Pharmaceuticals
Amdoxovir (DAPD)	nucleoside analogue RT inhibitor	Phase I/II	Triangle Pharmaceuticals
Alovudine (MIV-310, FLT)	nucleoside analogue RT inhibitor	Phase II	Medivir
ACH-126,443 (L-Fd4C)	nucleoside analogue RT inhibitor	Phase I	Achillion
SPD 756 (BCH-13520)	nucleoside analogue RT inhibitor	Phase I	Shire Biochem
SPD 754 (BCH-10618, DOTC)	nucleoside analogue RT inhibitor	Phase I	Shire Biochem
Phosphazid°	nucleoside analogue RT inhibitor	Preclinical	Viscount
Beta-D-Fd4C°	nucleoside analogue RT inhibitor	Preclinical	Vion
Beta-L-Fd4C°	nucleoside analogue RT inhibitor	Preclinical	Vion
BEA-005°	nucleoside analogue RT inhibitor	Preclinical	Medivir
Tenofovir	nucleotide analogue RT inhibitor	Approved	Gilead Sciences
Delavirdine	non-nucleoside RT inhibitor	Approved	Agouron
Nevirapine	non-nucleoside RT inhibitor	Approved	Boehringer Ingelheim
Efavirenz	non-nucleoside RT inhibitor	Approved	Bristol-Myers Squibb
Capravirine	non-nucleoside RT inhibitor	Phase III	Agouron
AI-183 (DPC083)	non-nucleoside RT inhibitor	Phase II	Bristol-Myers Squibb
Calanolide A	non-nucleoside RT inhibitor	Phase II	Sarawak Medichem
TMC 120**	non-nucleoside RT inhibitor	Phase II	Tibotec
TMC 125	non-nucleoside RT inhibitor	Phase II	Tibotec
DPC961°°	non-nucleoside RT inhibitor	Phase I	Bristol-Myers Squibb
MIV-150	non-nucleoside RT inhibitor	Phase I	Medivir/Chiron
PNU 142721	non-nucleoside RT inhibitor	Preclinical	Pharmacia
RD4-2217	non-nucleoside RT inhibitor	Preclinical	Tosoh
SJ-3366	non-nucleoside RT inhibitor	Preclinical	Samjin
UC-781	non-nucleoside RT inhibitor	Preclinical	Biosyn
HI-236	non-nucleoside RT inhibitor	Preclinical	Wayne Hughes Institute
MV026048	non-nucleoside RT inhibitor	Preclinical	Hoffman LaRoche / Medivir
Saquinavir	protease inhibitor	Approved	Hoffman-La Roche
Indinavir	protease inhibitor	Approved	Merck
Ritonavir	protease inhibitor	Approved	Abbott
Nelfinavir	protease inhibitor	Approved	Agouron/Pfizer
Amprenavir	protease inhibitor	Approved	Vertex/GlaxoSmithKline
Lopinavir	protease inhibitor	Approved	Abbott
Atazanavir	protease inhibitor	Phase III	Bristol-Myers Squibb
VX-175/ GW433908 (amprenavir pro-drug)	protease inhibitor	Phase II/III	Vertex/GlaxoSmithKline
Tipranavir	protease inhibitor	Phase II	Boehringer Ingelheim
TMC 114	protease inhibitor	Phase I	Tibotec
DPC681°°	protease inhibitor	Preclinical	Bristol-Myers Squibb
DPC684°°	protease inhibitor	Preclinical	Bristol-Myers Squibb
LB-71350°	protease inhibitor	Preclinical	LG Chemical
Hydroxyurea	inhibits cellular factors	Phase II/III	Bristol-Myers Squibb
Mycophenylate	inhibits cellular factors	Phase I/II	Hofmann-La Roche
Peldesine	inhibits cellular factors	Phase I	Biocryst
Resveratrol	inhibits cellular factors	Phase I	Pharmascience
DEHSPM	inhibits hypusin / eIF-5A	Phase I	SunPharm
AXD455	inhibits eIF-5A	Phase I/II	Axxima Pharmaceuticals
Azodicarbonamide (ADA)	zinc finger inhibitor	Phase I/II	Hubriphar
ACH-100,076	zinc finger inhibitor	Preclinical	Achillion
Pentafuside (T-20)*	fusion inhibitor	Phase III*	Trimeris/Roche
T-1249	fusion inhibitor	Phase I	Trimeris/Roche
SCH C (SCH 351125)	CCR5 antagonist	Phase I	Schering Plough
UK-427,857	CCR5 antagonist	Phase I	Pfizer
TAK 449	CCR5 antagonist	Preclinical	Takeda
PRO 140	CCR5 antagonist	Preclinical	Progenics
SCH D	CCR5 antagonist	Preclinical	Schering Plough
AMD-3465°	CXCR4 antagonist	Preclinical	AnorMed
PRO367	entry inhibitor	Phase I	Progenics
BMS 806	entry inhibitor	Preclinical	Bristol-Myers Squibb
AMD-8664°	entry inhibitor	Preclinical	AnorMed
PRO 542	attachment inhibitor	Phase I/II	Progenics
S1360	integrase inhibitor	Phase I/II	Shionogi/GlaxoSmithKline
Hu5A8°	binding inhibitor	Preclinical	Tanox
HGTV43	antisense	Phase I/II	Enzo
Z-100	increase MIP-1alpha production	Phase I	Zeria

* Available in expanded access
° No information available
**Now being developed as a backup compound
°° Status unknown

• ABC: Abacavir
• APV: Amprenavir
• AUC: area under the curve, a measure of exposure to a drug; see PK
  bid: twice a day (dosing)
• Cmax: maximum concentration of a drug; see PK
• Cmin: minimum concentration of a drug; see PK
• DAIDS: Division of AIDS in National Institute of Allergy and Infectious Diseases
• DLV: Delavirdine
• DSMB: Data Safety Monitoring Board; review of ongoing clinical trial
• EAP: Expanded access program (for unapproved drugs)
• EC50: 50% effective concentration; see PK
• EC95: 95% effective concentration; see PK
• EFV: Efavirenz
• FDA: Food and Drug Administration (US drug approval agency); see overview of drug approval process at http://www.fda.gov/cder/handbook/dev_rev.htm
• Hx: history (patient medical history)
• IC50: 50% inhibitory concentration; see PK
• IC95: 95% inhibitory concentration; see PK
• IDV: Indinavir
• IND: Investigational New Drug (application); part of FDA approval process
• IRB: Institutional Review Board; one step in approval of a clinical trial
• LPV: Lopinavir (in Kaletra®)
• NDA: New Drug Application; part of FDA approval process
• NFV: Nelfinavir
• NIAID: National Institute of Allergy and Infectious Diseases (US)
• NNRTI: Non-nucleoside reverse transcriptase inhibitor, "non-nuke"
• NRTI: Nucleoside reverse transcriptase inhibitor, "nuke"
• NVP: Nevirapine
• OAR: Office of AIDS Research in the office of the Director of the National Institutes of Health
• PK: pharmacokinetics; study of how drugs are processed by the body. A review article is at http://www.thebody.com/gmhc/issues/julaug01/primer.html
• qd: once a day (dosing)
• RTV: Ritonavir
• RIT: Ritonavir
• SQV: Saquinavir
• TAM: Thymidine analog mutation, mutations in HIV reverse transcriptase that are significantly associated with resistance to thymidine analog drugs
• tid: three times a day (dosing)
• Tx: Treatment
• T½: Half-life (time for drug level to fall by 50%); see PK
• ZDV: zidovudine (AZT)

Revised June 11, 2002

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