Cabotegravir

Cabotegravir Uses, Dosage, Side Effects, Food Interaction and all others data.

Cabotegravir, or GSK1265744, is an HIV-1 integrase inhibitor that is prescribed with the non-nucleoside reverse transcriptase inhibitor, rilpivirine. Early research into cabotegravir showed it had lower oral bioavailability than dolutegravir. The devlopment of cabotegravir was later developed to create a long acting monthly intramuscular injection.

Cabotegravir was granted FDA approval on 21 January 2021.

Cabotegravir is an inhibitor of HIV integrase, which reduces viral replication. It has a long duration of action as the oral tablet is given daily and the intramuscular suspension is given monthly. Patients should be counselled regarding the risk of hypersensitivity, hepatotoxicity, and depression.

Cabotegravir
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Cabotegravir
Availability	Prescription only
Generic	Cabotegravir
Cabotegravir Other Names	Cabotegravir
Related Drugs	Biktarvy, Descovy, Truvada, tenofovir, ritonavir, emtricitabine / tenofovir, Complera, Atripla, Stribild, Apretude
Weight	30mg
Type	Oral tablet
Formula	C₁₉H₁₇F₂N₃O₅
Weight	Average: 405.358 Monoisotopic: 405.113626985
Protein binding	Cabotegravir is >99.8% bound to proteins in plasma, usually alubmin.
Groups	Approved, Investigational
Therapeutic Class
Manufacturer
Available Country	United States
Last Updated:	September 19, 2023 at 7:00 am

Uses

Cabotegravir is an HIV-1 integrase inhibitor.

Oral cabotegravir is indicated in combination with rilpivirine for the short term treatment of HIV-1 in virologically suppressed adults with no history of treatment failure to assess tolerability of cabotegravir or who have missed an injected dose of cabotegravir. Intramuscular extended-release cabotegravir is indicated in combination with rilpivirine as a complete regimen for virologically suppressed adults with no history of treatment failure. The intramuscular form is meant to replace their current antiretroviral treatment.

Cabotegravir is also used to associated treatment for these conditions: Human Immunodeficiency Virus Type 1 (HIV-1)

How Cabotegravir works

Cabotegravir binds to the active site of HIV integrase, preventing strand transfer of the viral genome into the host genome, and preventing replication of the virus.

Toxicity

Data regarding the toxicity of cabotegravir is not readily available. In the event of overdose, patients should have their vital signs monitored, including an ECG to monitor the QT interval. Treat patients symptomatically and supportively. As cabotegravir is highly protein bound, dialysis is not expected to remove a significant amount of the drug from plasma.

Food Interaction

Take at the same time every day. Take the oral tablets at the same time every day.
Take with food. Take the oral tablets with a meal.

Cabotegravir multivitamins interaction

[Major] ADJUST DOSING INTERVAL: Coadministration with antacids, mineral supplements, or other medications containing polyvalent cations such as magnesium, aluminum, calcium, and iron may decrease the bioavailability of oral cabotegravir.

The proposed mechanism involves chelation of cabotegravir by polyvalent cations, forming a complex that is poorly absorbed from the gastrointestinal tract.

The interaction has not been studied with cabotegravir, but has been reported with other integrase strand transfer inhibitors (INSTIs).

To minimize the risk of reduced viral susceptibility and resistance development associated with subtherapeutic levels of cabotegravir, medications containing polyvalent cations such as antacids and mineral supplements should be administered at least 2 hours before or 4 hours after the oral cabotegravir dose.

Cabotegravir Drug Interaction

Unknown: bictegravir / emtricitabine / tenofovir alafenamide, mycophenolate mofetil, tadalafil, doravirine / lamivudine / tenofovir, emtricitabine / tenofovir alafenamide, fluorouracil topical, cobicistat / elvitegravir / emtricitabine / tenofovir, emtricitabine / tenofovir, acetaminophen, sildenafil

Cabotegravir Disease Interaction

Moderate: depression, liver impairment, renal impairment

Volume of Distribution

Data regarding the volume of distribution of cabotegravir is not readily available.

Elimination Route

Oral cabotegravir has a T_max of 3 hours, reaches a C_max of 8.0 µg/mL, and has an AUC of 145 µg*h/mL. Intramuscular extended-release cabotegravir has a T_max of 7 days, reaches a C_max of 8.0 µg/mL, and has an AUC of 1591 µg*h/mL.

Half Life

The mean half life of oral cabotegravir is 41 hours. The mean half life of intramuscular extended-release cabotegravir is 5.6-11.5 weeks.

Clearance

Data regarding the clearance of cabotegravir is not readily available. Clearance in dogs was 0.34 mL/min/kg and in cynomolgus monkeys was 0.32 mL/min/kg.