"目录号: HY-15287A
Anti-infectionMetabolic Enzyme/Protease-
Nelfinavir(AG-1341)是口服的人HIV-1蛋白酶抑制剂，Ki为2nM。
HIVHIV Protease
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Dolutegravir-Maraviroc-Elvitegravir-Atazanavir sulfate-Tenofovir Disoproxil Fumarate-Tipranavir-Triciribine-Emtricitabine-Efavirenz-Miltefosine-Ritonavir-Delavirdine mesylate-Lamivudine-Abacavir-BI 224436-
生物活性
Description
Nelfinavir(AG-1341) is a potent and orally bioavailable human immunodeficiency virus HIV-1 protease inhibitor (Ki=2 nM) and is widely prescribed in combination with HIV reverse transcriptase inhibitors for the treatment of HIV infection. IC50 Valur: 2 nM (Ki for HIV-1 protease) [2]Target: HIV Proteasein vitro: In vitro exposure (72 hours) of HAECs to NEL (0.25-2 μg/mL) decreased both basal (2.5-fold) and insulin-induced NO production (4- to 5-fold). NEL suppressed insulin-induced phosphorylation of both Akt and eNOS at serine residues 473 and 1177, respectively. NEL decreased tyrosine phosphorylation of IR-β, IRS-1, and PI3K. Coexposure to troglitazone (TRO; 250 nM) ameliorated the suppressive effects of NEL on insulin signaling and NO production. Coexposure to TRO also increased eNOS expression in NEL-treated HAECs [1]. AG1343 is a potent enzyme inhibitor (Ki = 2 nM) and antiviral agent (HIV-1 ED50 = 14 nM). An X-ray cocrystal structure of the enzyme-AG1343 complex reveals how the novel thiophenyl ether and phenol-amide substituents of the inhibitor interact with the S1 and S2 subsites of HIV-1 protease, respectively [2].in vivo: In vivo studies indicate that AG1343 is well absorbed orally in a variety of species and possesses favorable pharmacokinetic properties in humans [2].
Clinical Trial
NCT00704600
Maastricht Radiation Oncology
Colorectal Cancer-Colorectal Carcinoma-Colorectal Tumors-Neoplasms, Colorectal
September 2008
Phase 1-Phase 2
NCT02080416
Sidney Kimmel Comprehensive Cancer Center
Non-Hodgkin Lymphoma-Hodgkin Lymphoma-Kaposi Sarcoma-Gastric Cancer-Nasopharyngeal Cancer-EBV-Castleman Disease
July 2014
Early Phase 1
NCT03077451
AIDS Malignancy Consortium-National Cancer Institute (NCI)-The EMMES Corporation-University of Arkansas-University of California, Los Angeles-AIDS and Cancer Specimen Resource
Recurrent Kaposi Sarcoma-Skin Kaposi Sarcoma
March 13, 2017
Phase 2
NCT01925378
Joseph Anthony Lucci III-The University of Texas Health Science Center, Houston
Cervical Dysplasia
July 2012
Phase 2
NCT01065844
University of Iowa-Holden Comprehensive Cancer Center
Carcinoma, Adenoid Cystic-Head and Neck Neoplasms
October 2009
Phase 2
NCT02066311
Northwell Health-National Institute of Arthritis and Musculoskeletal and Skin Diseases (NIAMS)
Systemic Lupus Erythematosus
September 2014
Phase 2
NCT01079286
Academisch Medisch Centrum - Universiteit van Amsterdam (AMC-UvA)
Renal Cell Cancer-Cancer
June 2009
Phase 1
NCT01447589
Oxford University Hospitals NHS Trust
Lung Cancer
February 2012
Phase 1-Phase 2
NCT01728779
Sidney Kimmel Comprehensive Cancer Center
Oligometastases
April 2013
Phase 2
NCT00791336
University of Iowa
Carcinoma, Non-Small-Cell Lung
August 2008
Phase 2
NCT00694837
Maastricht Radiation Oncology-Maastricht University Medical Center
Glioblastoma
March 2009
Phase 1
NCT00246610
Pfizer
HIV Infection
March 2006
Phase 4
NCT01555281
Swiss Group for Clinical Cancer Research
Multiple Myeloma
April 2012
Phase 1-Phase 2
NCT00205283
University of Wisconsin, Madison-Agouron Pharmaceuticals
HIV Infections
August 2003
NCT01086332
University of Iowa-Holden Comprehensive Cancer Center
Pancreatic Neoplasms
May 2009
Phase 1
NCT02188537
Swiss Group for Clinical Cancer Research
Myeloma
December 2014
Phase 2
NCT01445106
National Cancer Institute (NCI)-National Institutes of Health Clinical Center (CC)
Solid Tumors
December 11, 2006
Phase 1
NCT00251030
Pfizer-Jasper Clinic, Michigan
Healthy Volunteers
November 2005
Phase 4
NCT01485731
University of Miami
Cervical Cancer
January 2012
Phase 1
NCT01164709
Swiss Group for Clinical Cancer Research
Leukemia-Lymphoma-Mature T-cell and Nk-cell Neoplasms-Multiple Myeloma and Plasma Cell Neoplasm
July 2010
Phase 1
NCT00023400
Centers for Disease Control and Prevention-VA Office of Research and Development
HIV Infections-Tuberculosis
February 2000
Phase 4
NCT03050060
University of Washington-National Cancer Institute (NCI)
Metastatic Renal Cell Cancer-Recurrent Melanoma-Recurrent Non-Small Cell Lung Carcinoma-Recurrent Renal Cell Carcinoma-Stage IV Non-Small Cell Lung Cancer-Stage IV Renal Cell Cancer-Stage IV Skin Melanoma
June 9, 2017
Phase 2
NCT01108666
Abramson Cancer Center of the University of Pennsylvania
Non Small Cell Lung Cancer
March 2010
Phase 1
NCT00141284
Pfizer
HIV Infection-Hepatitis C
October 2005
Phase 4
NCT00312182
Pfizer
Healthy Volunteers
March 2006
Phase 4
NCT00002165
Agouron Pharmaceuticals-NIH AIDS Clinical Trials Information Service
HIV Infections
NCT00346619
Mayo Clinic
Immune Response
October 2005
Phase 1
NCT00002201
Abbott
HIV Infections
NCT01020292
Abramson Cancer Center of the University of Pennsylvania
Glioma
April 2009
Phase 1
NCT00002164
Agouron Pharmaceuticals-NIH AIDS Clinical Trials Information Service
HIV Infections
Phase 1
NCT00002375
Merck Sharp & Dohme Corp.-NIH AIDS Clinical Trials Information Service
HIV Infections
NCT00233948
City of Hope Medical Center
Adult Liposarcoma-Recurrent Adult Soft Tissue Sarcoma-Stage III Adult Soft Tissue Sarcoma-Stage IV Adult Soft Tissue Sarcoma
March 2006
Phase 1-Phase 2
NCT00915694
Abramson Cancer Center of the University of Pennsylvania-National Cancer Institute (NCI)
Brain and Central Nervous System Tumors
April 2009
Phase 1
NCT02207439
Abramson Cancer Center of the University of Pennsylvania
Stage III, IVa, or IVb Squamous Cell Carcinoma of the Oral Cavity, Oropharynx, Larynx, or Hypopharynx
July 2014
Phase 2
NCT00650637
Pfizer
Diarrhea
January 2003
Phase 3
NCT00002171
Agouron Pharmaceuticals-NIH AIDS Clinical Trials Information Service
HIV Infections
Phase 2
NCT00002185
Agouron Pharmaceuticals-NIH AIDS Clinical Trials Information Service
Sarcoma, Kaposi-HIV Infections
Phase 2
NCT02363829
Abramson Cancer Center of the University of Pennsylvania
Uterine Cervix Cancer
February 2015
Phase 1
NCT00002169
Agouron Pharmaceuticals-NIH AIDS Clinical Trials Information Service
Cytomegalovirus Retinitis-HIV Infections
Phase 2
NCT00000893
National Institute of Allergy and Infectious Diseases (NIAID)-Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)
HIV Infections
October 1997
Phase 1
NCT00002170
Agouron Pharmaceuticals-NIH AIDS Clinical Trials Information Service
Mycobacterium Avium-Intracellulare Infection-HIV Infections
Phase 2
NCT01068327
University of Nebraska-National Cancer Institute (NCI)
Adenocarcinoma of the Pancreas-Stage III Pancreatic Cancer
November 2007
Phase 1
NCT00028067
Bristol-Myers Squibb
HIV Infections
August 2001
Phase 3
NCT00002381
Boehringer Ingelheim-NIH AIDS Clinical Trials Information Service
HIV Infections
Phase 1
NCT00000898
National Institute of Allergy and Infectious Diseases (NIAID)
HIV Infections
NCT00146380
Centers for Disease Control and Prevention
HIV Infections
July 2003
Phase 2
NCT00589056
Abramson Cancer Center of the University of Pennsylvania-National Cancer Institute (NCI)