AVAILABLE MEDICINE FOR Bictegravir


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Introduction to Bictegravir

Bictegravir is a antiretroviral medication used for treating HIV-1 infection. It is part of a group of drugs called integrase strand transfer inhibitors (INSTIs). These drugs stop the virus from inserting its genetic material into the DNA of host cells, preventing replication. 

Its development began in the early 2010 as researchers sought to create more effective and tolerable HIV treatments. Bictegravir is often used with other antiretroviral medications to create a complete treatment plan, which has greatly improved patient health and quality of life.


Chemical Properties of Bictegravir

Bictegravir has a complex structure that effectively blocks the HIV integrase enzyme. Its molecular formula is C21H18F3N3O5S. 

It usually comes in tablet form and is combined with other antiretroviral drugs for better treatment results. Bictegravir is a crystalline solid that works best when paired with other medications.


How it Works ?

Bictegravir stops the HIV integrase enzyme, which is essential for the virus to replicate. This enzyme integrates viral DNA into the host cell's genome. By blocking this process, Bictegravir prevents the virus from spreading and replicating, making it crucial for managing HIV-1 infection.


Effectiveness

Bictegravir has shown high effectiveness in clinical trials, significantly lowering viral loads and increasing CD4 cell counts in patients. Over 90% of patients maintained viral suppression after 48 weeks of treatment. 

This high success rate highlights Bictegravir's importance in HIV therapy. It has also been compared positively with other antiretrovirals like dolutegravir, showing similar or better effectiveness and tolerability.


Regulatory Approval  

The U.S. Food and Drug Administration (FDA) approved Bictegravir for use in combination with emtricitabine and tenofovir alafenamide in February 2018. This approval marked a significant milestone, as Biktarvy became a preferred first-line therapy for HIV-1 infection due to its robust efficacy and favorable safety profile.


Dosage and Administration 

Dosage Instructions -  The usual dose of Bictegravir is 50 mg. It is often taken with emtricitabine and tenofovir alafenamide in one tablet. Take it once a day, with or without food, for best results.


Administration Tips

  • Take the tablet at the same time each day to keep drug levels steady in your body.
  • If you miss a dose, take it as soon as you remember.
  • Do not take two doses at once to make up for a missed one.
  • Skipping doses or taking too much can affect how well the treatment works and may lead to drug resistance.

Side Effect of Bictegravir

Common Side Effects:

  • Nausea

  • Diarrhea

  • Headache

  • Fatigue

Serious Side Effects (Less Common):

  • Liver toxicity

  • Lactic acidosis

Drug Interactions and Precautions

Medications to Avoid or Use with Caution:

  • Certain anticonvulsants

  • Specific antibiotics

  • Herbal supplements such as St. John’s Wort

Precautions:

  • Always inform your healthcare provider about any other medications or supplements you are using.

  • Use caution when combining Bictegravir with drugs that influence the CYP3A4 enzyme.

  • Interactions with these substances may affect the efficacy and metabolism of Bictegravir.

Current Research and Developments in Bictegravir

In 2017, bictegravir was included in a fixed-dose combination tablet with emtricitabine and tenofovir alafenamide, branded as Biktarvy. This combination was aimed at simplifying HIV treatment regimens while maintaining high efficacy.


  • Expanded Drug Combinations Research. 

They are testing Bictegravir with new drugs and optimizing its use with existing ones to improve results and lessen side effects.Researchers are looking at new ways to combine Bictegravir with other HIV drugs to make treatment more effective and reduce resistance. 


  • Pre-Exposure Prophylaxis (PrEP) 

Scientists are studying Bictegravir as part of PrEP to prevent HIV infection. They want to see how well Bictegravir works in stopping HIV transmission in high-risk groups, which is important as the need for effective prevention grows.


  • Hepatitis B and C Co-Infection

Research is examining how Bictegravir can help patients who have both HIV and hepatitis B or C. The goal is to see if Bictegravir can effectively manage HIV in these patients and improve treatment strategies.


  • Resistance and Genotypic Testing 

Researchers are studying how well Bictegravir works against new HIV strains and drug resistance. They are using genotypic testing to customize treatment based on individual viral profiles, which helps improve Bictegravir's effectiveness.


  • Alternative Delivery Methods

Investigations are underway to find new ways to deliver Bictegravir, such as long-acting injections. These studies aim to make it easier for patients to stick to their treatment plans and manage HIV more conveniently.


Refrences:


https://www.drugs.com/history/biktarvy.html

https://www.ema.europa.eu/en/medicines/human/EPAR/biktarvy

https://www.thelancet.com/journals/lanchi/article/PIIS2352-4642(21)00165-6/abstract

https://www.gilead.com/news-and-press/press-room/press-releases/2024/4/fda-approves-biktarvy-label-update-with-data-for-pregnant-adults-with-hiv