lenacapavir

Actions and spectrum: 

lenacapavir is a medication that is being developed for the treatment of HIV infection. It is a capsid inhibitor, which means it targets a specific protein (called the capsid) that is essential for the virus to replicate. By inhibiting the capsid, lenacapavir prevents the virus from reproducing and spreading throughout the body. 

One of the most attractive features of lenacapavir is its broad-spectrum antiviral activity. It is active against a wide variety of HIV-1 strains, including those that are resistant to other antiretroviral medications. This is important because HIV can quickly mutate and become resistant to the drugs used to treat it, making it a difficult virus to combat. 

 

DRUG INTERACTION

Contraindicated  

Serious Use Alternative  

Monitor Closely  

Minor  

Frequency defined

10%: 

Injection site reactions 

1-10%: 

Nausea 

Glycosuria 

Proteinuria 

Hyperglycemia 

 

Black Box Warnings: 

The black box warning for lenacapavir states that the drug should not be used in combination with other antiretroviral medications, as it has not been studied in combination with other drugs and may lead to drug interactions or reduced effectiveness. Additionally, it is recommended that patients with certain genetic mutations associated with resistance to other antiretroviral medications should not receive lenacapavir. 

Contraindication / Caution: 

Contraindication: 

• Lenacapavir is contraindicated in patients with known hypersensitivity to lenacapavir or any of its excipients. 

Caution: 

• Patients with a history of Class III or IV congestive heart failure should use lenacapavir with caution. 
• Lenacapavir may interact with certain medications, such as rifampin, which may reduce its effectiveness. Therefore, it should be used with caution in patients taking other medications. 
• It is not known if lenacapavir is safe and effective in children under 18 years of age. Therefore, it should be used with caution in this population. 
• Patients with severe renal impairment should use lenacapavir with caution, as the safety and efficacy of lenacapavir in this population have not been established. 
• Women who are pregnant or breastfeeding should consult with their healthcare provider before starting lenacapavir, as the safety of the drug in these populations has not been established. 

 

 

 

Pregnancy consideration:  

Insufficient data is available regarding the use of the drug in pregnant females. 

Breastfeeding warnings:  

No data is available regarding the excretion of the drug in breast milk. 

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies do not show risk to the fetus in the first/later trimester.        
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women        
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.       
• Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.        
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.        
• Category N: There is no data available for the drug under this category 

Pharmacology 

lenacapavir is an antiviral drug that is being developed for the treatment of HIV-1 infection. It belongs to a class of drugs known as capsid inhibitors, which target the viral capsid protein that is essential for the viral replication process. 

lenacapavir works by binding to the viral capsid protein and disrupting its structure, which prevents the virus from entering host cells and replicating. This results in the inhibition of viral replication and the reduction of viral load in the body. 

Pharmacodynamics 

lenacapavir is a viral capsid inhibitor that is used to treat HIV-1 infections. It works by binding to a specific site on the viral capsid protein and inhibiting the formation of the viral core, which is essential for viral replication. This binding also causes structural changes in the capsid protein that lead to the disruption of the virus’s ability to infect new cells. 

lenacapavir is highly selective for HIV-1, with little to no activity against other viruses or host cells. It has a high barrier to resistance, as mutations that would allow the virus to escape the drug’s effects would likely be lethal to the virus. 

Overall, the pharmacodynamics of lenacapavir involve binding to the viral capsid protein and inhibiting the formation of the viral core, leading to a disruption of the virus’s ability to infect new cells and a significant reduction in viral load in patients with HIV-1 infection. 

Pharmacokinetics 

Absorption: 

The bioavailability of lenacapavir is 6-10% after oral administration and 100% after subcutaneous