nelfinavir
Trade name: viracept
Approved
Mar 14, 1997
Nelfinavir is a protease inhibitor with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Protease inhibitors block the part of HIV called protease. HIV-1 protease is an enzyme required for the proteolytic cleavage of the viral polyprotein precursors into the individual functional proteins found in infectious HIV-1. Nelfinavir binds to the protease active site and inhibits the activity of the enzyme. This inhibition prevents cleavage of the viral polyproteins resulting in the formation of immature non-infectious viral particles. Protease inhibitors are almost always used in combination with at least two other anti-HIV drugs. Nelfinavir inhibits the HIV viral proteinase enzyme which prevents cleavage of the gag-pol polyprotein, resulting in noninfectious, immature viral particles. Nelfinavir is used in combination with other antiviral drugs in the treatment of HIV in both adults and children. Nelfinavir is marketed under the brand name Viracept. — NCATS
Clinical trial activity
135 trials · 71 clinical orgs · 2 marketing orgs
Earliest trial started May 1, 1997 (NCT00002177)
Timeline
1990s
2000s
- Apr 30, 2003
Pfizer — NDA Secondary Org
Indications
Approved for
Studied for
- AIDS-Associated Nephropathy · Phase 3
- Brain Neoplasms · Phase 1
- Carcinoma, Adenoid Cystic · Phase 2
- Carcinoma, Non-Small-Cell Lung · Phase 2
- Carcinoma, Renal Cell · Phase 2
- Carcinoma, Squamous Cell · Phase 2
- Cardiopulmonary Bypass · Phase 1
- Cardiovascular Diseases · Phase 4
- Castleman Disease · Early Phase 1
- Colorectal Neoplasms · Phase 1/Phase 2
- Cytomegalovirus Retinitis · Phase 2
- Diarrhea · Phase 3
- Endometrial Neoplasms · Phase 1
- Glioblastoma · Phase 1
- Glioma · Phase 1
- Head and Neck Neoplasms · Phase 2
- Healthy Volunteers · Phase 4
- Hepatitis C · Phase 4
- Herpesvirus 4, Human · Early Phase 1
- HIV · Phase 3
- HIV-Associated Lipodystrophy Syndrome · Phase 4
- HIV Seronegativity · Phase 1
- Hodgkin Disease · Early Phase 1
- Immunity · Phase 1
- Infectious Disease Transmission, Vertical · Phase 3
- Kidney Neoplasms · Phase 2
- Leukemia · Phase 1
- Lipodystrophy · Phase 4
- Liposarcoma · Phase 1/Phase 2
- Lung Neoplasms · Phase 1/Phase 2
- Lupus Erythematosus, Systemic · Phase 2
- Lymphoma · Phase 1
- Lymphoma, Non-Hodgkin · Early Phase 1
- Melanoma · Phase 2
- Multiple Myeloma · Phase 2
- Mycobacterium avium-intracellulare Infection · Phase 2
- Nasopharyngeal Neoplasms · Early Phase 1
- Neoplasm Metastasis · Phase 2
- Neoplasms · Phase 1/Phase 2
- Ovarian Neoplasms · Phase 2
- Pancreatic Neoplasms · Phase 2
- Pregnancy · Phase 3
- Sarcoma · Phase 2
- Sarcoma, Kaposi · Phase 2
- Sepsis · Phase 1
- Squamous Cell Carcinoma of Head and Neck · Phase 2
- Stomach Neoplasms · Early Phase 1
- Tuberculosis · Phase 4
- Uterine Cervical Dysplasia · Phase 2
- Uterine Cervical Neoplasms · Phase 3
- Vulvar Neoplasms · Phase 1
Mechanism of action
Q72874 inhibitor
Approval history
- approvedPriority reviewAcceleratedMar 14, 1997
Chemistry & pharmacology
SMILES
Cc1c(O)cccc1C(=O)N[C@@H](CSc1ccccc1)[C@H](O)CN1C[C@H]2CCCC[C@H]2C[C@H]1C(=O)NC(C)(C)C- Mol. weight
- 567.8 g/mol
- Lipinski Ro5
- 1 violation(s)
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL584 ↗
- WikipediaNelfinavir ↗
- NCATSHO3OGH5D7I ↗
- ChEMBLCHEMBL1205 ↗
Also known as
- ag-1343
- ag-1343
- nelfinavir
- nelfinavir
- nelfinavir
- nelfinavir
- nelfinavir
- nelfinavir
- nelfinavir
- nelfinavir
- nelfinavir
- nelfinavir
- nelfinavir
- nelfinavir
- nelfinavir mesilate
- nelfinavir mesilate
- nelfinavir mesilate
- nelfinavir mesylate
- nelfinavir mesylate
- nelfinavir mesylate
- nelfinavir mesylate
- viracept
- viracept
- viracept
- viracept
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT06971744 | Phase 2 | Jan 1, 2026 | Medical University of South Carolina |
| NCT07281781 | Phase 1/Phase 2 (Phase 2) | Sep 16, 2025 | Chao Family Comprehensive Cancer Center, University of California, Irvine |
| NCT05036226 | Phase 1/Phase 2 (Phase 2) | Jan 15, 2022 | Medical University of South Carolina |
| NCT04169763 | Phase 1 | Mar 30, 2020 | National Cancer Institute (NCI), University of Texas at Houston |
| NCT03829020 | Phase 1 | Apr 17, 2019 | Mayo Clinic, National Cancer Institute (NCI) |
| NCT03631732 | Phase 3 | Aug 28, 2018 | Gilead Sciences |
| NCT03256916 | Phase 3 | Sep 25, 2017 | Tata Memorial Hospital |
| NCT03050060 | Phase 2 | Jun 9, 2017 | National Cancer Institute (NCI), University of Washington |
| NCT03077451 | Phase 2 | Mar 13, 2017 | AIDS and Cancer Specimen Resource, AIDS Malignancy Consortium, Hoosier Cancer Research Network, National Cancer Institute (NCI), The EMMES Corporation, University of California, Los Angeles |
| NCT03422874 | Phase 1 | Aug 31, 2016 | Dartmouth University |
| NCT02024009 | Phase 1/Phase 2 (Phase 2) | Mar 1, 2016 | Cancer Research UK, Celgene, University of Oxford |
| NCT02363829 | Phase 1 | Feb 1, 2015 | University of Pennsylvania |
| NCT02858401 | Phase 1 | Jan 29, 2015 | Gilead Sciences |
| NCT02188537 | Phase 2 | Dec 1, 2014 | Cantonal Hospital of St. Gallen, Swiss Group for Clinical Cancer Research |
| NCT02066311 | Phase 2 | Sep 1, 2014 | National Institute of Arthritis and Musculoskeletal and Skin Diseases (NIAMS), Northwell Health |
| NCT02080416 | Early Phase 1 (Phase 1) | Jul 1, 2014 | Johns Hopkins University |
| NCT02207439 | Phase 2 | Jul 1, 2014 | University of Pennsylvania |
| NCT01959672 | Phase 2 | Sep 1, 2013 | National Cancer Institute (NCI), University of Nebraska |
| NCT01728779 | Phase 2 | Apr 1, 2013 | Johns Hopkins University |
| NCT01925378 | Phase 2 | Jul 1, 2012 | The University of Texas Health Science Center, Houston, University of Texas at Houston |
Organizations
Research & Development (71)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| National Institute of Allergy and Infectious Diseases (NIAID) | Government | 35 | 34 | 4 | 1997 |
| Agouron | For profit | 15 | 12 | 5 | 1999 |
| National Cancer Institute (NCI) | Government | 10 | 1 | 2 | 1997 |
| National Institutes of Health (NIH) | Government | 10 | 1 | 4 | 1997 |
| Glaxo Wellcome | For profit | 9 | 8 | 5 | 1999 |
| Bristol-Myers Squibb | For profit | 8 | 7 | 4 | 1997 |
| Roche | For profit | 7 | 6 | 4 | 1999 |
| University of Pennsylvania | Academic/Hospital | 6 | 6 | 2 | 2007 |
| Gilead Sciences | For profit | 5 | 5 | 3 | 1999 |
| Pfizer | For profit | 5 | 5 | 2 | 2003 |
| Mayo Clinic | Academic/Hospital | 4 | 4 | 1 | 2003 |
| Merck | For profit | 4 | 4 | 2 | 1999 |
| Cantonal Hospital of St. Gallen | Academic/Hospital | 3 | 0 | 2 | 2010 |
| Swiss Group for Clinical Cancer Research | Academic/Hospital | 3 | 3 | 2 | 2010 |
| University of Iowa | Academic/Hospital | 3 | 3 | 2 | 2008 |
| University of Washington | Academic/Hospital | 3 | 1 | 2 | 2002 |
| Abbott | For profit | 2 | 2 | 2 | 1999 |
| AIDS Malignancy Consortium | Academic/Hospital | 2 | 1 | 1 | 1997 |
| Boehringer Ingelheim | For profit | 2 | 2 | 1 | 1999 |
| Duke University | Academic/Hospital | 2 | 0 | 2 | 1999 |