Bioequivalence Study of Generic GPO Saquinavir and Norvir® Versus Invirase® and Norvir®

Bioequivalence Study of Generic GPO Saquinavir and Norvir® Versus Invirase® and Norvir® in Thai Healthy Volunteers

The previous two studies of generic GPO saquinavir failed to prove bioequivalence. In this study the bio-equivalence will be investigated in healthy Thai volunteers, to see whether the generic GPO saquinavir shows bioequivalence when boosted with Norvir®. If the generic formulation is bioequivalent subsequent studies may follow in HIV-1 positive patients.

Study Overview

• Status: Withdrawn
• Conditions: HIV Infections
• Intervention / Treatment: Drug: generic GPO saquinavir and novir vs invirase and norvir

Detailed Description

The primary objective is to establish bioequivalence of "ritonavir boosted generic GPO saquinavir", with Invirase® and Norvir® as the reference drug.

The secondary objective is to evaluate the short-term tolerability and safety profiles of generic saquinavir in healthy male volunteers.

• Study Type: Interventional
• Phase: Phase 2; Phase 1

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 45 years (Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: All

Description

Inclusion Criteria:

• Written informed consent
• Healthy male 18-45 years old
• Documented negative test for HIV-1 infection < 1 wk prior to start of study and with no risk of HIV exposure in the last 6 months
• BMI 18-25
• Normal physical examination
• Normal CBC, BUN, Cr, AST, ALT, Total bilirubin, no evidence of active or chronic HBV or HCV infection

Exclusion Criteria:

• History of sensitivity/idiosyncrasy to the drug or chemically related compounds or excipients, which may be employed in the study.
• Relevant history or current condition that might interfere with drug absorption, distribution, metabolism or excretion.
• Inability to understand the nature and extent of the study and the procedures required.
• Participation in a drug study within 60 days prior to the first dose.
• Febrile illness within 3 days before the first dose.
• Use of concomitant medication
• Smoke cigarettes not more than 10 cigarettes a day.
• Drink alcohol not more than 2 units a day.
• Discontinue smoking and alcohol for at least 1 month before enrollment.
• Take other medication regularly
• Involvement in any drug addiction.
• Heart disease, hypertension, liver disease, kidney disease, GI disease, allergic disease or other diseases which may interfere with the PK of study drugs

Study Plan

How is the study designed?

Design Details

• Allocation: Randomized
• Interventional Model: Crossover Assignment
• Masking: None (Open Label)

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Active Comparator: A; Day 1: receive a single dose of Invirase®/Norvir® 1,000 mg / 100mg 7-day washout period will follow. Day 8: take generic GPO squinavir/Norvir	Drug: generic GPO saquinavir and novir vs invirase and norvir; Norvir® 100mg capsules, Invirase® 1,000 mg capsules Generic GPO Saquinavir 1,000 mg capsules For phase 1 and 2 - At day 1 subjects of group A will receive a single dose of Invirase®/Norvir® 1,000 mg / 100mg, while group B will receive generic GPO saquinavir / Norvir® 1,000 mg / 100mg as single dose. The same day the first 24 hr PK curve will be done. After this, a 7-day washout period will follow. At day 8 group A will take generic GPO saquinavir / Norvir® and Group B will take Invirase®/Norvir®. At this day, the second 24 hr PK curve will be done
Active Comparator: B; Day 1: take generic GPO squinavir/Norvir 7-day washout period will follow. Day 8: receive a single dose of Invirase®/Norvir® 1,000 mg / 100mg	Drug: generic GPO saquinavir and novir vs invirase and norvir; Norvir® 100mg capsules, Invirase® 1,000 mg capsules Generic GPO Saquinavir 1,000 mg capsules For phase 1 and 2 - At day 1 subjects of group A will receive a single dose of Invirase®/Norvir® 1,000 mg / 100mg, while group B will receive generic GPO saquinavir / Norvir® 1,000 mg / 100mg as single dose. The same day the first 24 hr PK curve will be done. After this, a 7-day washout period will follow. At day 8 group A will take generic GPO saquinavir / Norvir® and Group B will take Invirase®/Norvir®. At this day, the second 24 hr PK curve will be done

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
To establish bioequivalence of ritonavir boosted generic GPO saquinavir generic, with Invirase® and Norvir® as reference drug.	8 days

Secondary Outcome Measures

Outcome Measure	Time Frame
The secondary objective is to evaluate the short-term tolerability and safety profiles of generic saquinavir in healthy male volunteers.	8 days

Collaborators and Investigators

• Sponsor: The HIV Netherlands Australia Thailand Research Collaboration
• Collaborators: The Government Pharmaceutical Organization
• Investigators: Principal Investigator: Kiat Ruxrungtham, MD, The HIV Netherlands Australia Thailand Research collaboration (HIV-NAT)

Publications and helpful links

Helpful Links

• The HIV Netherlands Australia Thailand Research Collaboration (HIV-NAT)

Study record dates

Study Registration Dates

• First Submitted: February 12, 2008
• First Submitted That Met QC Criteria: February 21, 2008
• First Posted (Estimate): February 22, 2008

Study Record Updates

• Last Update Posted (Estimate): March 26, 2015
• Last Update Submitted That Met QC Criteria: March 24, 2015
• Last Verified: March 1, 2015

More Information

Terms related to this study

• Keywords: pharmacokinetics; bioequivalence; ritonavir boosted generic GPO saquinavir; saftey
• Additional Relevant MeSH Terms: RNA Virus Infections; Virus Diseases; Infections; Blood-Borne Infections; Communicable Diseases; Sexually Transmitted Diseases, Viral; Sexually Transmitted Diseases; Lentivirus Infections; Retroviridae Infections; Immunologic Deficiency Syndromes; Immune System Diseases; HIV Infections; Molecular Mechanisms of Pharmacological Action; Anti-Infective Agents; Antiviral Agents; Enzyme Inhibitors; Anti-HIV Agents; Anti-Retroviral Agents; Protease Inhibitors; Cytochrome P-450 CYP3A Inhibitors; Cytochrome P-450 Enzyme Inhibitors; HIV Protease Inhibitors; Viral Protease Inhibitors; Saquinavir
• Other Study ID Numbers: HIV-NAT 038