Current status of anti

Drug Type	Brand Name Links to simple fact sheets from AIDS Treatment Data Network	Generic	Chemical Name or Identifier	Clinical Stage in US (July 1999)	Manufacturer (link to manufacturer data sheet or other information)	Other Links +	Misc	NIAID database structure
Drugs that inhibit the HIV protease
Protease inhibitor	Crixivan	indinavir		Approved	Merck			here
Protease inhibitor	Invirase	saquinavir (hard gel)		Approved	Hoffmann- La Roche			here
Protease inhibitor	Fortovase	saquinavir (soft gel)		Approved	Hoffmann- La Roche			here
Protease inhibitor	Norvir	ritonavir		Approved	Abbott	Body		here
Protease inhibitor	Viracept	nelfinavir		Approved	Hoffman La Roche/ Agouron			here
Protease inhibitor	Agenerase Prozei	amprenavir	141W94/VX-478	Approved	Glaxo- Wellcome	DG Body		here
Protease inhibitor		lopinavir	ABT-378	Phase III Likely to file for FDA approval in 2000	Abbott	H+H	News	here
Protease inhibitor		tripanavir	PNU-140690	Phase II	Pharmacia & Upjohn		Non-peptide inhibitor based on a dihydropyrone template. Synergizes with Ritonavir	here
Protease inhibitor			BMS-232632	Phase I/II	Bristol-Myers Squibb		Azapeptide protease inhibitor
Protease inhibitor			DMP-450	Phase I	Triangle		Novel cyclic urea compound	here
Protease inhibitor			L756423	Phase II	Merke		May delay resistance with AZT
Protease inhibitor			AG1776		Agouron		Maintains activity against strains of HIV resistant to current protease inhibitors
Protease inhibitor			GW433908 (VX-175)		Glaxo Wellcome and Vertex		A "prodrug" form of amprenavir. A prodrug becomes active after it is broken down in the body.
Drugs that are DNA chain terminators and competitive inhibitors of reverse transcriptase
Nucleoside RT inhibitor	Combivir *	zidovudine +lamivudine		Approved	Glaxo- Wellcome	H&H
Nucleoside RT inhibitor	Epivir	lamivudine	3TC	Approved	Glaxo- Wellcome			here
Nucleoside RT inhibitor	Hivid	zalcitabine	ddC	Approved	Hoffman- La Roche			here
Nucleoside RT inhibitor	Retrovir	zidovudine	AZT	Approved	Glaxo- Wellcome			here
Nucleoside RT inhibitor	Videx	didanosine	ddI	Approved	Bristol-Myers Squibb			here
Nucleoside RT inhibitor	Zerit	stavudine	d4T	Approved	Bristol-Myers Squibb			here
Nucleoside RT inhibitor	Ziagen	abacavir	1592U89	Approved	Glaxo- Wellcome			here
Nucleoside RT inhibitor	Preveon	adefovir dipivoxil	PMEA	Phase II/III	Gilead Sciences	Body H&H	Acyclic nucleotide analog. Anti-viral activity not high; may be useful in combination therapy. Nephrotoxicity a problem. Must be taken with carnitine.	here
Nucleoside RT inhibitor		tenofovir	PMPA	Phase II	Gilead Sciences		Acyclic nucleotide analog. Does not need carnitine and no nephrotoxicity. Well tolerated. Good anti-viral activtity	here
Nucleoside RT inhibitor	Coviracil	emtricitabine	FTC	Phase II/III	Triangle			here
Nucleoside RT inhibitor			DAPD (DXG)	Phase I/II	Triangle
Nucleoside RT inhibitor		lodenosine	F-ddA	Phase II. Withdrawn - adverse events	US Bioscience	+ve		here
Nucleoside RT inhibitor			dOTC (BCH-10652)	Phase I/II			Well tolerated
Drugs that are non-competitive inhibitors of reverse transcriptase
Non-nucleoside RT inhibitor	Rescriptor	delavirdine		Approved	Pharmacia & Upjohn			here
Non-nucleoside RT inhibitor	Viramune	nevirapine		Approved	Boeringer Ingelheim			here
Non-nucleoside RT inhibitor	Sustiva	efavirenz	DMP-266	Approved	DuPont- Merck	H&H	Mechanism More info	here
Non-nucleoside RT inhibitor	Coactinon	emivirine	MKC-442	Phase II/III	Triangle
Non-nucleoside RT inhibitor			S-1153	Phase II	Agouron			here
Non-nucleoside RT inhibitor			DPC 961, 963, 082, 083	Phase I/II	Du Pont		Potent and better tolerated than Sustiva
Non-nucleoside RT inhibitor			GW420867X	Phase I	Glaxo-Wellcome
Non-nucleoside RT inhibitor	Calanolide A			Phase I Phase II at end of 1999	Sarawak Medichem		Natural product - derived from a plant (Calophyllum lanigerum). Other calanolides being tested	here
Drugs that are inhibitors of the integrase
	Zintevir		AR-177	Phase I/II human trials.	Aronex Pharmaceuticals		Phase I trials showed that the drug is well tolerated. Zintevir belongs to a class of novel oligo- nucleotides. It is a short (17-mer) G-T-containing polynucleotide
Zintevir was first tested in 1998 and was thought to be an integrase inhibitor. However, while it may inhibit purified integrase in tests in the laboratory,this does not appear how it works against HIV in vivo. The drug appears to prevent the binding of gp120 to CD4 cells. This finding that Zintevir probably does not act as an integrase inhibitor in cells does not affect its possible value as an HIV inhibitor.
Drugs that are anti-sense inhibitors
			HGTV43	Phase I	Enzo Therapeutics,		Mechanism Press release
Drugs that interact with the surface glycoprotein of HIV
Gp120 competitor			PRO-542	Phase I/II	Progenics		A fusion protein of HIV-binding region of CD4 and a human antibody. It binds to gp120 and neutralizes it by preventing virus from binding to the cell surface or detaching gp120 from the HIV envelope, thereby inactivating the virus
Gp120 competitor			PRO-367	PhaseI/II	Progenics		Radioimmuno-conjugate similar to PRO-542 that binds to HIV-infected cells and kills them via radio-therapeutic radioisotope
Drugs that stop the fusion of the viral envelope with the host cell membrane
Fusion Inhibitor			AMD-3100	Phase I/II	AnorMED		Synthetic molecule that blocks the "CXCR4" receptor on CD4 cells. The drug is administered by injection.
Fusion Inhibitor			FP21399	Phase I trial as a single infusion or a series of 4 weekly 1-hour intravenous infusions.	Fuji Pharmaceuticals		The drug produced viral load decreases and CD4+ cell increases. Side effects were minor, including blue-tinted urine and temporary blue marks on the skin.
Fusion Inhibitor			T-1249	Phase I	Trimeris		T-1249 is effective against HIV that is resistant to T-20.
Fusion Inhibitor			T-20	Phase II	Trimeris- Hoffmann LaRoche		Mechanism Mechanism Mechanism 36 amino acid synthetic peptide that binds to a key region of surface protein, gp41. Blocks HIV viral fusion by interfering with structural rearrangements with gp41 that are required for HIV to fuse to and enter ahost cell.
Fusion Inhibitor			T-1249	Phase I/II	Trimeris		39 amino acid peptide that binds to a region of the HIV gp41 surface protein that differs from the region bound by T-20.


Other drugs
Therapeutic Vaccine	Remune	immunogen		Phase III Trial stopped (Go here) New trial planned	Agouron/ Immune Response		More info