Why are more and more HIV patients choosing self funded integrase inhibitor drugs?

Why are more and more HIV patients choosing to pay for themselves
The replication process of HIV-1 in human cells includes four stages: attachment and entry, reverse transcription and integration, transcription and translation, maturation and budding. Integrase, reverse transcriptase and protease are three enzymes necessary for AIDS infected cells to replicate.
Previously, anti AIDS drugs used in clinical practice were all targeted at reverse transcriptase or protease, but the problems such as large adverse reactions and susceptibility to drug resistance of such drugs are increasingly affecting patients, so more and more researchers are beginning to use integrase (IN) as a target for developing new antiviral drugs.
The integration process in the HIV replication cycle is the process of integrating HIV-1 DNA into host DNA, and it is also an indispensable process in the HIV-1 replication cycle.
HIV-1 integrase participates in the entire integration process, catalyzes the entire integration reaction, and helps retroviruses integrate DNA carrying viral genetic information into host DNA. It is an essential key enzyme in the replication cycle of HIV virus and an indispensable enzyme for stable viral infection. And integrases are usually carried by the virus itself, and there are no integrase functional analogues in the human body.
HIV integrase inhibitors (INSTI), also known as HIV integrase chain transfer inhibitors, can effectively inhibit HIV replication in the body by inhibiting HIV integrase, without harming normal cells. Therefore, they have high selectivity and low toxicity.
The safety of integrase inhibitors is significantly higher than that of non nucleoside and protease inhibitors, and the adverse reactions in the central nervous system are significantly reduced compared to EFV. The adverse reactions in blood lipids and digestive system are better than protease inhibitors. Moreover, it also has the advantages of rapid virus reduction, high drug resistance barrier, less toxic side effects, and high compliance. Since its listing, it has received a lot of praise. Since 2016, it has become the preferred recommendation in AIDS treatment guidelines in various countries. In August 2018, Professor Lu Hongzhou, an infectious disease expert at the Shanghai Public Health Clinical Center, officially released the “Expert Consensus on the Clinical Application of integrase inhibitors”, benefiting more domestic patients.
Integrase inhibitor
The main integrase inhibitors currently available on the market are:
Raltegravir (RAL)
Latiravir can simultaneously inhibit the replication of HIV-1 and HIV-2. The drug resistance barrier is low and there is cross resistance with EVG. Its effectiveness is due to the use of atazanavir/ritonavir (ATV/r) and darunavir/ritonavir (DRV/r), which have high medication safety and no food restrictions during the medication period. However, the drug resistance barrier is lower than that of DTG and BIC, and pregnant women who take DTG simultaneously during pregnancy are at risk of developing neural tube defects in their infants. It is stronger and causes milder side effects than other previously known integrase inhibitors.
Elvitegravir (EVG)
The drug resistance barrier is low, and there is cross resistance with RAL. It requires the use of agonists for administration and requires co consumption with food; The resistance barrier is relatively lower compared to DTG and BIC; Due to the inhibition of creatinine secretion in renal tubules, it can lead to an increase in blood creatinine; Due to insufficient blood drug concentration in pregnant women, it should be avoided for use in pregnant women.
Dolutegravir (DTG)
The drug resistance barrier is high, there is less cross resistance, and the efficacy is better than RAL. There are also single agent preparations that can be used in combination with other drugs; The interaction between drugs is relatively small, and there are no food restrictions during the medication period. However, due to the inhibition of creatinine secretion by DTG in renal tubules, it can lead to an increase in blood creatinine; High incidence of insomnia and headache during medication period; In addition, pregnant women who take DTG during pregnancy are at risk of developing neural tube defects in their infants.
Bictegravir (BIC, not yet approved in China)
The drug resistance barrier is relatively high and there is less cross resistance. The advantage is that the risk of virological failure and drug resistance is low, and HLA * B5701 does not need to be tested during use. There are no food restrictions during medication. However, there is currently limited clinical use and insufficient data on various adverse reactions.
In addition, there are fixed dose compound formulation Stribild and the under development long-acting formulation cabotegravir (CAB).
Antiviral regimen containing integrase inhibitors
Antiviral treatment regimen containing integrase inhibitors
The 2018 World Health Organization (WHO) guidelines recommend DTG+2NRTIs as the preferred option for initial treatment patients, as well as the preferred second-line option for adults or children after treatment failure; Recommend TDF+3TC (FTC) as the preferred backbone regimen, DTG as the preferred third drug, among which TAF has better renal and skeletal safety than TDF.
In the next few years, compound single tablets with integrase inhibitors as the core will become the mainstream of treatment!