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Pathway Description
Bictegravir Action Pathway
Homo sapiens
Drug Action Pathway
Bictegravir is an integrase inhibitor used to treat HIV-1 and HIV-2 infections. Bictegravir is indicated in the management of HIV-1 infection in patients not previously treated with antiretroviral therapy. Additionally, Bictegravir is indicated in the management of HIV-1 infection in patients who are virologically suppressed (HIV-1 RNA <50 c/mL) on a regular antiretroviral regimen for a minimum of three months without a history of failure in treatment and no known factors associated with the resistance to the individual components of the medication. In vitro, bictegravir has shown powerful antiviral activity against HIV-2 and various subtypes of HIV-1. It is used in combination with tenofovir and emtricitabine.
Bictegravir is transported into the infected cell then transported into the nucleus via importin nuclear transporter. The viral RNA is injected into the cell then transcribed into viral DNA via reverse transcriptase. It is then transported into the nucleus where it is integrated into the host DNA. Bictegravir inhibits HIV integrase which prevents the viral DNA from being integrated into the host DNA. This prevents viral replication and further progression of the virus. It is used in combination with reverse transcriptase inhibitors which further prevents viral replication and progression of the virus.
References
Bictegravir Pathway References
Deepthi A, Raju S, Kalyani A, Udaya Kiran M, Vanaja A. Targeted Drug Delivery to the Nucleus and its Potential Role in Cancer Chemotherapy. J. Pharm. Sci. & Res., v. 2013;5(2):48–56.
Chase SP, Freimanis AK: Abdominal echography. Ohio State Med J. 1971 Oct;67(10):901-6.
Pubmed: 5118987
Gallant JE, Thompson M, DeJesus E, Voskuhl GW, Wei X, Zhang H, White K, Cheng A, Quirk E, Martin H: Antiviral Activity, Safety, and Pharmacokinetics of Bictegravir as 10-Day Monotherapy in HIV-1-Infected Adults. J Acquir Immune Defic Syndr. 2017 May 1;75(1):61-66. doi: 10.1097/QAI.0000000000001306.
Pubmed: 28196003
https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/210251s014lbl.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/210251s015lbl.pdf
Wishart DS, Feunang YD, Guo AC, Lo EJ, Marcu A, Grant JR, Sajed T, Johnson D, Li C, Sayeeda Z, Assempour N, Iynkkaran I, Liu Y, Maciejewski A, Gale N, Wilson A, Chin L, Cummings R, Le D, Pon A, Knox C, Wilson M: DrugBank 5.0: a major update to the DrugBank database for 2018. Nucleic Acids Res. 2018 Jan 4;46(D1):D1074-D1082. doi: 10.1093/nar/gkx1037.
Pubmed: 29126136
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