Cobicistat: Difference between revisions

Cobicistat
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Latest revision as of 00:52, 20 February 2025

A pharmacokinetic enhancer used in antiretroviral therapy

Cobicistat is a pharmacokinetic enhancer used in combination with other antiretroviral drugs for the treatment of HIV/AIDS. It is not active against HIV itself but enhances the effectiveness of other drugs by inhibiting the cytochrome P450 3A (CYP3A) enzymes, which are responsible for the metabolism of many antiretroviral drugs.

Mechanism of Action[edit]

Cobicistat works by inhibiting the CYP3A enzymes in the liver and intestines. This inhibition leads to increased plasma concentrations of drugs that are metabolized by these enzymes, such as atazanavir and darunavir. By boosting the levels of these drugs, cobicistat allows for lower doses to be used, reducing the potential for side effects and improving patient adherence to therapy.

Clinical Use[edit]

Cobicistat is used as a component of fixed-dose combination therapies for the treatment of HIV-1 infection. It is commonly found in combination with other antiretrovirals such as elvitegravir, emtricitabine, and tenofovir. These combinations are used in once-daily regimens that simplify treatment and improve adherence.

Pharmacokinetics[edit]

Cobicistat is absorbed in the gastrointestinal tract and reaches peak plasma concentrations approximately 3 to 4 hours after oral administration. It is extensively metabolized in the liver, primarily by CYP3A and CYP2D6 enzymes, and is excreted in the feces and urine.

Side Effects[edit]

Common side effects of cobicistat include nausea, diarrhea, and fatigue. It can also cause increases in serum creatinine due to inhibition of renal tubular secretion, which may lead to reduced kidney function in some patients. Monitoring of renal function is recommended during treatment.

Drug Interactions[edit]

Due to its mechanism of action, cobicistat can interact with a wide range of drugs that are metabolized by CYP3A enzymes. It is important to review a patient's medication list for potential interactions and adjust dosages accordingly.

Related pages[edit]

Cobicistat

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-{{intro}}
+{{Short description|A pharmacokinetic enhancer used in antiretroviral therapy}}
-Cobimetinib is a tyrosine kinase receptor inhibitor that is used in combination with vemurafenib as therapy for selected forms of advanced malignant melanoma.
+{{Drugbox
+| image = Cobicistat_structure.svg
+| image_size = 200px
+| image_alt = Structural formula of Cobicistat
+| image_caption = Structural formula of Cobicistat
+}}
-{{livtox}}
+'''Cobicistat''' is a pharmacokinetic enhancer used in combination with other antiretroviral drugs for the treatment of [[HIV/AIDS]]. It is not active against HIV itself but enhances the effectiveness of other drugs by inhibiting the [[cytochrome P450]] 3A (CYP3A) enzymes, which are responsible for the metabolism of many antiretroviral drugs.
-The combination of cobimetinib and vemurafenib is commonly associated with serum enzyme elevations during therapy and to rare instances of clinically apparent acute liver injury.
-{{moa}}
+==Mechanism of Action==
-Cobimetinib (koe" bi me' ti nib) is a small molecule tyrosine kinase receptor inhibitor with potent activity against the mitogen-activated extracellular regulated kinase (MEK), which is an important component of the kinase cascade in the mitogen activated protein kinase (MAPK) pathway (RAS-RAF-MEK-ERK).  Components of the MAPK pathways are frequently mutated in patients with malignant melanoma, particularly the RAF isoform BRAF.  BRAF-mutations cause a constitutive activation of the MAPK pathways, resulting in unregulated cell growth and proliferation.  Inhibition of MEK has been found to be synergistic when combined with specific BRAF inhibitors as therapy of BRAF-mutated cancers.  Clinical trials have shown that the addition of cobimetinib with vemurafenib (a specific BRAF-kinase inhibitor) results in improvements in survival in patients with melanoma who harbor the V600 BRAF mutation.
+Cobicistat works by inhibiting the CYP3A enzymes in the liver and intestines. This inhibition leads to increased plasma concentrations of drugs that are metabolized by these enzymes, such as [[atazanavir]] and [[darunavir]]. By boosting the levels of these drugs, cobicistat allows for lower doses to be used, reducing the potential for side effects and improving patient adherence to therapy.
-{{fda}}
+==Clinical Use==
-Cobimetinib received accelerated approval for use as combination therapy with vemurafenib in the United States in 2015.  Current indications are as combination therapy of metastatic or unresectable melanoma with BRAF V600E or V600K mutations.
+Cobicistat is used as a component of fixed-dose combination therapies for the treatment of HIV-1 infection. It is commonly found in combination with other antiretrovirals such as [[elvitegravir]], [[emtricitabine]], and [[tenofovir]]. These combinations are used in once-daily regimens that simplify treatment and improve adherence.
-{{dose}}
+==Pharmacokinetics==
-Cobimetinib is available in tablets of 20 mg under the brand name Cotellic.  The recommended dose is 60 mg once daily for the first 21 days of each 28-day cycle, continued until disease progression or intolerable toxicity occurs.
+Cobicistat is absorbed in the gastrointestinal tract and reaches peak plasma concentrations approximately 3 to 4 hours after oral administration. It is extensively metabolized in the liver, primarily by CYP3A and CYP2D6 enzymes, and is excreted in the feces and urine.
-{{se}}
+==Side Effects==
-Side effects are common and include diarrhea, rash, photosensitivity, nausea, stomatitis, fever, alopecia and thrombocytopenia.  Uncommon, but potentially severe side effects include severe diarrhea leading to dehydration and renal failure, rhabdomyolysis, cardiac toxicity, retinal detachment and embryo-fetal toxicity.
+Common side effects of cobicistat include nausea, diarrhea, and fatigue. It can also cause increases in serum creatinine due to inhibition of renal tubular secretion, which may lead to reduced kidney function in some patients. Monitoring of renal function is recommended during treatment.
-{{cancer drugs}}
-{{coststubd}}
+==Drug Interactions==
+Due to its mechanism of action, cobicistat can interact with a wide range of drugs that are metabolized by CYP3A enzymes. It is important to review a patient's medication list for potential interactions and adjust dosages accordingly.
+==Related pages==
+* [[HIV/AIDS]]
+* [[Antiretroviral drug]]
+* [[Cytochrome P450]]
+* [[Pharmacokinetics]]
+[[Category:Antiretroviral drugs]]
+[[Category:Pharmacokinetic enhancers]]
+<gallery>
+File:Cobicistat structure.svg|Cobicistat
+</gallery>