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saquinavir

Phase 3

HIV Infections | Small molecule | Infectious Disease |Roche Holding AG|Last Updated: Mar 29, 2018

Success Probability

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Trial Design

RandomizedDouble-BlindCONTROLLED
Total Trials11
Total Enrollment8,861

FDA Designations

No designations recorded

Clinical trial landscape

saquinavir · 11 trials · 1 indication

Phase 3 4Phase 2 5Phase 1 2
NCT00105079GEMINI Study - A Study of Saquinavir/Ritonavir in Treatment-Naive Patients With HIV-1 InfectionHIV Infections
COMPLETED337 Analytics
NCT00002334A Study of Zidovudine (AZT) Used Alone or in Combination With Other Anti-HIV Drugs in HIV-Infected Patients With Little or No Previous TreatmentHIV Infections
COMPLETED3,000 Analytics
NCT00002367A Study of Saquinavir Soft Gelatin Capsules Plus Zidovudine Plus Lamivudine in the Treatment of HIV-1 Infected Patients Who Have Never Taken Anti-HIV DrugsHIV Infections
COMPLETED40 Analytics
NCT00002382A Study of Saquinavir Used Alone or in Combination With Other Anti-HIV Drugs in HIV-Infected PatientsHIV Infections
COMPLETED4,000 Analytics
PHASE3COMPLETED
GEMINI Study - A Study of Saquinavir/Ritonavir in Treatment-Naive Patients With HIV-1 Infection
HIV InfectionsUnlock trial analytics
PHASE3COMPLETED
A Study of Zidovudine (AZT) Used Alone or in Combination With Other Anti-HIV Drugs in HIV-Infected Patients With Little or No Previous Treatment
HIV InfectionsUnlock trial analytics
PHASE3COMPLETED
A Study of Saquinavir Soft Gelatin Capsules Plus Zidovudine Plus Lamivudine in the Treatment of HIV-1 Infected Patients Who Have Never Taken Anti-HIV Drugs
HIV InfectionsUnlock trial analytics
PHASE3COMPLETED
A Study of Saquinavir Used Alone or in Combination With Other Anti-HIV Drugs in HIV-Infected Patients
HIV InfectionsUnlock trial analytics

Study Endpoints

Primary Endpoints

Number of Patients With Human Immunodeficiency Virus Type 1 (HIV-1) Ribonucleic Acid (RNA) Viral Load <50 Copies/mL
Week 48

The primary objective of this study was to evaluate the efficacy of saquinavir/ritonavir BID plus emtricitabine/tenofovir QD versus lopinavir/ritonavir BID plus emtricitabine/tenofovir QD in treatment-naïve HIV-1 infected adults. Blood samples for HIV-1 RNA viral load measurement were collected at the Week 48 clinic visit. The number of participants with HIV-1 RNA results \<50 copies/mL is reported.

Plasma Trough Concentrations (Ctrough) for Saquinavir
Pre-dose at Weeks 8, 12, 24.

Plasma trough concentration is the average steady state concentration prior to morning and evening dose. Ctrough of Saquinavir was normalized to a dose of 50 mg/kg.

Area Under the Plasma Concentration-time Curve Over the Time Interval From Zero to Twelve Hours (AUC0-12h) for Saquinavir
Pre-dose and 3, 4, 8, 12 hours (post-dose) on Day 14 (± 2 days), or Day 28(+ 2 days) for patients switching from an Non-nucleoside reverse transcriptase inhibitor [NNRTI] containing regimen).

The area under the plasma concentration-time curve from time zero to twelve hours (AUC0-12h) is area under the plasma concentration-time curve from time zero through actual tlast. The area under the plasma concentration-time curve from time zero to twelve hours of saquinavir was normalized to a dose of 50 mg/kg.

Incidence of Adverse Events (AE) and Serious Adverse Events (SAE)
From Baseline (Day 1) till Week 48 and Follow-up (Week 52)

An AE is defined as any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. An SAE is defined as any untoward medical occurrence that, at any dose, results in death, is life threatening, requires hospitalization or prolongation of existing hospitalization, results in persistent or significant disability/incapacity, is a congenital anomaly/birth defect, or is a significant medical event in the investigator's judgment or requires intervention to prevent one or other of these outcomes

Change In Hematocrit From Baseline
Baseline (Day 1), Week 24 and Week 48

Change from Baseline was calculated as the post-Baseline value minus the Baseline value.

Change In Hemoglobin, Total Protein And Total Albumin From Baseline
Baseline (Day 1), Week 24 and Week 48

Change from Baseline was calculated as the post-Baseline value minus the Baseline value.

Change In White Blood Cell (WBC), Platelet, Basophil, Lymphocyte, Monocyte, Neutrophil And Eosinophil Cell Counts From Baseline
Baseline (Day 1), Week 24 and Week 48

Change from Baseline was calculated as the post-Baseline value minus the Baseline value.

Change In Red Blood Cell (RBC) Counts From Baseline
Baseline (Day 1), Week 24 and Week 48

Change from Baseline was calculated as the post-Baseline value minus the Baseline value.

Change In Creatine Kinase (CK), Serum Glutamic Oxaloacetic Transaminase (SGOT), Alkaline Phosphatase (ALP), Serum Glutamic-Pyruvic Transaminase (SGPT), Gamma-Glutamyl Transferase (GGT) Counts From Baseline
Baseline (Day 1), Week 24 and Week 48

Change from Baseline was calculated as the post-Baseline value minus the Baseline value.

Change In Total Bilirubin, Creatinine, Uric Acid From Baseline
Baseline (Day 1), Week 24 and Week 48

Change from Baseline was calculated as the post-Baseline value minus the Baseline value.

Change In Blood Urea Nitrogen (BUN), Low Density Lipoprotein (LDL) Cholesterol, High Density Lipoprotein (HDL Cholesterol), Triglycerides, Calcium, Potassium, Sodium, Chloride, Phosphate, Fasting Glucose From Baseline
Baseline (Day 1), Week 24 and Week 48

Change from Baseline was calculated as the post-Baseline value minus the Baseline value.

Change In Hematuria, Glycosuria And Proteinuria From Baseline
Baseline (Day 1), Week 24 and Week 48

Change from Baseline was calculated as the post-Baseline value minus the Baseline value.

Area Under the Plasma Concentration-Time Curve From Time of Administration to 12 Hours After Dosing (AUC 0-12h) of Saquinavir (SQV) and Ritonavir (RTV)
Pre-dose and at 0.5 hr, 1hr, 2hrs, 3hrs, 4hrs, 5hrs, 6hrs, 8hrs, 10hrs, and 12 hrs post-dose on Day 14

Area Under the Plasma Concentration-Time Curve (AUC) is a measure of the plasma concentration of the drug over time. It is used to characterize drug absorption. The pharmacokinetic profile for following 14 days of administration with SQV/RTV 1000/100 mg BID included determining the area under the plasma concentration-time curve from 0 to 12 hours after dosing (AUC (0-12h) of SQV and RTV The AUC (0-12hours) was analyzed for SQV and RTV by non-compartmental methods, using WinNonlin.

Maximum Observed Plasma Concentration (Cmax) of SQV and RTV
Pre-dose and at 0.5 hr, 1hr, 2hrs, 3hrs, 4hrs, 5hrs, 6hrs, 8hrs, 10hrs, and 12 hrs post-dose on Day 14

The plasma concentration (Cmax) is defined as maximum observed analyte concentration. The pharmacokinetic profile for following 14 days of administration with SQV/RTV 1000/100 mg BID included determining the maximum observed plasma concentration (C max) of SQV and Ritonavir RTV The Cmax was analyzed for SQV and RTV by non-compartmental methods, using WinNonlin.

Secondary Endpoints

Number of Patients With HIV-1 RNA Viral Load <50 and <400 Copies/mL
Week 48
Change From Baseline in HIV-1 RNA Viral Load
Baseline to Week 48
Change From Baseline in Cluster Differentiation Antigen 4 Positive (CD4+) Lymphocyte Count
Baseline to Week 48
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Study Design & Arms

AllocationRANDOMIZED
MaskingNONE
ModelPARALLEL
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
saquinavir/ritonavirEXPERIMENTALsaquinavir mesylate 1000 mg twice daily (BID) + ritonavir 100 mg BID + emtricitabine/tenofovir disoproxil fumarate 200/300 mg orally every day for 48 weeks.
lopinavir/ritonavirACTIVE_COMPARATORlopinavir/ritonavir 400/100 mg BID + emtricitabine/tenofovir disoproxil fumarate 200/300 mg orally every day for 48 weeks.
1EXPERIMENTAL -
2EXPERIMENTAL -

Interventions

NameTypeDescription
saquinavir [Invirase]DRUG1000 milligram (mg) Oral (po) twice daily (bid)
Lopinavir/ritonavirDRUGLopinavir/ritonavir 400/100 mg po bid
Emtricitabine/tenofovir disoproxil fumarateDRUGEmtricitabine/tenofovir disoproxil fumarate 200/300 mg po qd
RitonavirDRUG100 mg po bid
SaquinavirDRUG -
ZidovudineDRUG -
ZalcitabineDRUG -
LamivudineDRUG -
StavudineDRUG -
DidanosineDRUG -
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Eligibility Criteria

Age Range18 Years to N/A
SexALL
Healthy VolunteersNo
Study Sites44

Inclusion Criteria: * adult patients \>=18 years of age; * chronic HIV-1 infection; * treatment-naive; * HIV-1 RNA viral load \>=10,000copies/mL; * women of childbearing potential must have a negative pregnancy test, and must use reliable contraception for the duration of the study and for 90 days ...

Countries:United StatesCanadaFrancePuerto RicoThailandArgentinaSpain
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Frequently asked questions about saquinavir

What is saquinavir used for?

Saquinavir is used for the treatment of HIV infections. It is a small molecule drug being developed by Roche Holding AG (ticker: RHHBY) and is currently in Phase 3 clinical development. Saquinavir is administered in combination with other antiretroviral drugs to manage HIV infection.

Who makes saquinavir?

Saquinavir is developed by Roche Holding AG, a pharmaceutical company traded under the ticker RHHBY. The drug is being investigated for the treatment of HIV infections and is currently in Phase 3 clinical development.

What phase is saquinavir in?

Saquinavir is in Phase 3 clinical development. It is an investigational drug for the treatment of HIV infections. While it has completed 11 clinical trials, it has not been reported as FDA approved, and its development status remains investigational.

What clinical trials is saquinavir in?

Saquinavir has been studied in 11 completed clinical trials with a total enrollment of 8,861 participants. Notable trials include NCT00002162, a Phase 2 study comparing two formulations of saquinavir in combination with other antiretrovirals, and NCT00623597, a Phase 2 study of saquinavir/ritonavir in HIV-infected infants and children.

Is saquinavir the same as Invirase?

Saquinavir is also known as Invirase. Clinical trials, such as NCT00623597, refer to Invirase (saquinavir) in their titles, confirming that Invirase is a brand name for saquinavir. The drug is being developed by Roche Holding AG for HIV infections.