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A Breif Drug Development Analysis of Antiretrovirals

Views: 31     Author: Unibest Industrial     Publish Time: 2023-09-26      Origin: Site

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Antiretroviral drugs have evolved significantly over time, with new drugs continuously being developed. The analysis below provides some insights into the development timeline, the focus on drug classes, and the use of drugs in combination formulations.


Evolution of Drug Classes

The following timeline summarizes the development of major drug classes over time:

1.  1980s-1990s: Early development of Nucleoside Reverse Transcriptase Inhibitors (NRTIs), the earliest class to be approved, such as Zidovudine (Retrovir) in 1987, followed by Abacavir (Ziagen) and Lamivudine (Epivir) in 1998 and 1995 respectively.

2.  1990s-2000s: Focus on the development of Non-nucleoside Reverse Transcriptase Inhibitors (NNRTIs) and Protease Inhibitors (PIs).

3.  Mid-2000s - Present: Intensive development of Integrase Strand Transfer Inhibitors (INSTIs) and a new wave of different drug classes such as Fusion Inhibitors, CCR5 Antagonists, and others.

It is important to note that the development of different drug classes has been primarily based on overcoming the limitations of previous drugs, as well as improving the effectiveness and reducing the side effects.


generic name drug class brand name approval date combinations
abacavir NRTIs Ziagen 1998/12/17 Epzicom, Triumeq, Triumeq PD, Trizivir
emtricitabine NRTIs Emtriva 2003/07/02 Biktarvy, Symtuza, Atripla, Genvoya, Stribild, Odefsey, Complera, Descovy, Truvada
lamivudine NRTIs Epivir 1995/11/17 Epzicom, Triumeq, Triumeq PD, Trizivir, Dovato, Delstrigo, Symfi, Symi Lo, Cimduo, Combivir
tenofovir disoproxil fumarate NRTIs Viread 2001/10/26 Delstrigo, Atripla, Stribild, Complera, Truvada, Cimduo
tenofovir alafenamide fumarate NRTIs

Biktarvy, Symtuza, Symfi, Symi Lo, Genvoya, Odefsey, Descovy
zidovudine NRTIs Retrovir 1987/03/19 Trizivir, Combivir
doravirine NNRTIs Pifeltro 2018/08/30 Delstrigo
efavirenz NNRTIs Sustiva 1998/09/17 Atripla, Symfi, Symi Lo
etravirine NNRTIs Intelence 2008/01/18
nevirapine NNRTIs Viramune 2011/03/25
extended-release nevirapine NNRTIs Viramune XR 2011/05/20
rilpivirine NNRTIs

Cabenuva, Juluca, Odefsey, Complera
atazanavir PIs Reyataz 2003/06/20 Evotaz
darunavir PIs Prezista 2006/06/23 Symtuza
fosamprenavir PIs Lexiva 2003/10/20
ritonavir PIs Norvir 1996/03/01 Kaletra
tipranavir PIs Aptivus 2005/06/22
opinavir PIs

Kaletra
enfuvirtide Fusion Inhibtors, g41 Fuzeon 2003/03/13
maraviroc CCR5 Antagonists Selzentry 2007/08/06
cabotegravir INSTIs Vocabria 2021/01/22 Cabenuva
dolutegravir INSTIs Trivicay 2013/08/12 Triumeq, Triumeq PD, Dovato, Juluca
dolutegravir sodium INSTIs Trivicay PD 2020/06/12
raltegravir INSTIs Isentress 2007/10/12
raltegravir potassium INSTIs Isentress HD 2017/05/26
elvitegravir INSTIs

Genvoya, Stribild
bictegravir INSTIs

Biktarvy
fostemsavir Fusion Inhibtors, gp120 Rukobia 2020/07/02
ibalizumab Post-attachment inhibitors, CD4 Trogarzo 2018/03/06
lenacapavir Capsid inhibitors Sunlenca 2022/12/22
cobicistat PK enhancers Tybost 2014/09/24 Evotaz, Symtuza, Genvoya


Use in Combination Formulations

NRTIs lead the charge in terms of combination formulations. Nearly every NRTI listed, such as Emtricitabine (Emtriva), Lamivudine (Epivir), and Tenofovir disoproxil fumarate (Viread), are used in multiple combination therapies.


INSTIs are also increasingly used in combination formulations, notably Dolutegravir (Trivicay) and Cabotegravir (Vocabria).

Anti-retroviral drug classes used in mixed drugs

Drug Class Distribution in Combination Formulations.png


Mostly Used Drugs in Combinations

Among all the drugs, Emtricitabine and Lamivudine are the two drug most frequently found in different combinations, suggesting a high versatility and effectiveness when it comes to treating HIV infection.

Ingredients used in mixed anti-retroviral drugs

Antiretroviral Drug in Combination Formulations.png


In conclusion, these insights suggest that while the focus has shifted from NRTIs towards more novel classes like INSTIs and capsid inhibitor, drugs from these early classes like NRTIs still play a key role, particularly in combination treatments. This probably indicates the efficacy of the drug in synergy with others and its continued relevance in the fight against HIV, despite the development of newer drug classes. However, this tendency for combinations also indicates the complexity of HIV treatment, underlining the need for a personalized and integrated treatment approach.


References