Selected Characteristics of Leading HIV-1 Protease Inhibitors

APPENDIX B
By Jules Levin, Executive Director of NATAP

Selected Characteristics of Leading HIV-1 Protease Inhibitors

Drug Name: Saquinavir Indinavir Ritonavir Nelfinavir 141W94 (VX-478)

Manufacturer: Merck Roche Abbott Agouron Glaxo-Wellcome Vertex

Status: Approved
(3/96) Approved
(12/95) Approved
(2/96) Phase III
Phase I/II

Synergy With: AZT, ddI, ddC,
d4T, 3TC AZT, ddI, ddC,
d4T, 3TC AZT, ddI, ddC,
d4T, 3TC AZT, ddI, ddC,
d4T, 3TC AZT, ddI, ddC, 1592U89
and other RT inhibitors

Patients To Date
(in Trials): >3,000 >2,100 >1,500 >500 <100

Bioavailability: 4% (with food) 40-60% 50-70% >50% (with food or fasted) >70%

Doses (mg/day): 1,800 mg 2,400 mg 1,200 mg 1,500 mg or 2,250 mg To Be Determined

Formulation: Oral capsule Oral capsule Oral semi-solid gel capsule Oral tablet Oral semi-solid gel capsule

Main Toxicities: Diarrhea Hyperbili-rubinemia, nephrolithiasis Nausea, vomiting, diarrhea, increases in liver enzymes, fasting triglycerides, and cholesterol Loose stool, diarrhea To Be Determined

Notes: Enhanced oral formulation with better bio-availability in development.
Delays emergence of AZT-resistant virus.
Delays disease progression and prolong survival.
Clinical endpoint studies ongoing.
Indinavir + enhanced oral formulation of saquinavir study is starting.
Indinavir + IL-2 data available.
Ritonavir + saquinavir exploratory study in progress (24 weeks in Jan `97).
Delays disease progression and prolong survival.
Preliminary pediatrics data available in NATAP Birmingham Report.
Six phase II/III studies in > 1,000 patients are ongoing.
Pediatric studies ongoing with powder formulation.
Neonates study planned.
Nelfinavir+ EOF saquinavir study planned.
Multiple drug interaction studies planned.
Pivotal trials are expected to enter clinics soon.
Planning combination studies with other protease inhibitors.
Expanded access program expected.

This document was written by Jules Levin, Executive Director of NATAP

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Drug Name:	Saquinavir	Indinavir	Ritonavir	Nelfinavir	141W94 (VX-478)
Manufacturer:	Merck	Roche	Abbott	Agouron	Glaxo-Wellcome Vertex
Status:	Approved (3/96)	Approved (12/95)	Approved (2/96)	Phase III	Phase I/II
Synergy With:	AZT, ddI, ddC, d4T, 3TC	AZT, ddI, ddC, d4T, 3TC	AZT, ddI, ddC, d4T, 3TC	AZT, ddI, ddC, d4T, 3TC	AZT, ddI, ddC, 1592U89 and other RT inhibitors
Patients To Date (in Trials):	>3,000	>2,100	>1,500	>500	<100
Bioavailability:	4% (with food)	40-60%	50-70%	>50% (with food or fasted)	>70%
Doses (mg/day):	1,800 mg	2,400 mg	1,200 mg	1,500 mg or 2,250 mg	To Be Determined
Formulation:	Oral capsule	Oral capsule	Oral semi-solid gel capsule	Oral tablet	Oral semi-solid gel capsule
Main Toxicities:	Diarrhea	Hyperbili-rubinemia, nephrolithiasis	Nausea, vomiting, diarrhea, increases in liver enzymes, fasting triglycerides, and cholesterol	Loose stool, diarrhea	To Be Determined
Notes:	Enhanced oral formulation with better bio-availability in development. Delays emergence of AZT-resistant virus. Delays disease progression and prolong survival.	Clinical endpoint studies ongoing. Indinavir + enhanced oral formulation of saquinavir study is starting. Indinavir + IL-2 data available.	Ritonavir + saquinavir exploratory study in progress (24 weeks in Jan `97). Delays disease progression and prolong survival. Preliminary pediatrics data available in NATAP Birmingham Report.	Six phase II/III studies in > 1,000 patients are ongoing. Pediatric studies ongoing with powder formulation. Neonates study planned. Nelfinavir+ EOF saquinavir study planned.	Multiple drug interaction studies planned. Pivotal trials are expected to enter clinics soon. Planning combination studies with other protease inhibitors. Expanded access program expected.