fostemsavir

an HIV-1 attachment inhibitor; structure in first source

Also Known As:

(3-((4-Benzoyl-1-piperazinyl)(oxo)acetyl)-4-methoxy-7-(3-methyl-1H-1,2,4-triazol-1-yl)-1H-pyrrolo(2,3-c)pyridin-1-yl)methyl dihydrogen phosphate; 1,2-Ethanedione, 1-(4-benzoyl-1-piperazinyl)-2-(4-methoxy-7-(3-methyl-1H-1,2,4-triazol-1-yl)-1-((phosphonooxy)methyl)-1H-pyrrolo(2,3-c)pyridin-3-yl)-; BMS-663068

Networked: 21 relevant articles (2 outcomes, 2 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Experts

1.	Ackerman, Peter: 6 articles (01/2022 - 01/2020)
2.	Llamoso, Cyril: 6 articles (01/2022 - 01/2020)
3.	Magee, Mindy: 4 articles (01/2022 - 01/2020)
4.	Moore, Katy: 4 articles (01/2022 - 01/2020)
5.	Lataillade, Max: 4 articles (11/2021 - 01/2014)
6.	Hanna, George J: 3 articles (10/2015 - 10/2012)
7.	Castagna, Antonella: 2 articles (01/2022 - 01/2020)
8.	Gartland, Margaret: 2 articles (11/2021 - 01/2020)
9.	Krystal, Mark: 2 articles (11/2021 - 10/2012)
10.	Pierce, Amy: 2 articles (11/2021 - 01/2020)

Related Diseases

1.	Infections 01/01/2014 - "Serious adverse events (SAEs) occurred in 13/200 (6.5%) and 5/51 (9.8%) subjects receiving BMS-663068 and ATV/r, respectively; most were secondary to infections and none were related to study drugs. " 01/01/2023 - "A computationally-assisted and green spectrophotometric method has been developed for the determination of fostemsavir, a recently FDA-approved drug used in combination with antiretroviral drugs to treat multidrug-resistant HIV-1 infection. " 04/01/2022 - "Fostemsavir for HIV-1 infection." 01/01/2022 - "Fostemsavir is the first attachment inhibitor approved by Food and Drug Administration and European Medicines Agency for the treatment of HIV-1 infection. " 01/01/2021 - "Fostemsavir may be an effective option for heavily treatment-experienced adults with multidrug-resistant HIV-1 infection. "
2.	Breast Neoplasms (Breast Cancer) 01/01/2022 - "Fostemsavir is a prodrug of temsavir, a first-in-class attachment inhibitor that binds directly to HIV-1 gp120, preventing initial viral attachment and entry into host CD4+ T cells with demonstrated efficacy in phase 2 and 3. Temsavir is a P-glycoprotein and breast cancer resistance protein (BCRP) substrate; its metabolism is mediated by esterase and CYP3A4 enzymes. "
3.	Chronic Kidney Failure (Chronic Renal Failure) 01/01/2023 - "The combination of lenacapavir plus fostemsavir looks promising in terms of safety and efficacy even in patients with end-stage renal disease awaiting renal transplant. " 01/01/2021 - "Overall, these results suggest that fostemsavir can be used without dose modification in subjects with mild to severe renal impairment, including those with end-stage renal disease on hemodialysis, and in subjects with mild to severe hepatic impairment."
4.	Headache (Headaches) 01/01/2014 - "The most common AE reported for BMS-663068 was headache (28/200, 14%), occurring in 5/51 (10%) subjects in the ATV/r arm; in the BMS-663068 arms, this was not dose-related. " 01/01/2021 - "The most common adverse reactions associated with fostemsavir use include nausea, diarrhea, headache, abdominal pain, dyspepsia, fatigue, rash, and sleep disturbance. "
5.	Abdominal Pain (Pain, Abdominal) 01/01/2021 - "The most common adverse reactions associated with fostemsavir use include nausea, diarrhea, headache, abdominal pain, dyspepsia, fatigue, rash, and sleep disturbance. "

Related Drugs and Biologics

1.	Prodrugs
2.	Cytochrome P-450 CYP3A
3.	Member 1 Subfamily B ATP Binding Cassette Transporter
4.	RNA (Ribonucleic Acid)
5.	Proteins (Proteins, Gene)
6.	Esterases
7.	Enzymes
8.	Anti-Retroviral Agents (Antiretroviral Agents)
9.	Ritonavir (Norvir)
10.	CD4 Antigens (CD4 Antigen)

Related Therapies and Procedures

1.	Therapeutics
2.	Highly Active Antiretroviral Therapy (HAART)
3.	Renal Dialysis (Hemodialysis)