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Only for medical professionals to read for reference.
The problem of HIV resistance should not be underestimated! AIDS is a serious infectious disease caused by the human immunodeficiency virus (HIV), and it is one of the serious public health challenges worldwide
.
HIV takes the most important CD4+ T lymphocytes in the human immune system as the main target and conducts large-scale destruction, ultimately destroying the patient's immune function, leading to fatal opportunistic infections and malignant tumors [1]
.
In recent years, the application of anti-retroviral therapy (ART) has made AIDS a chronic and controllable disease.
However, because HIV is a retrovirus, it has a high error rate and strong variability in the process of replication and evolution.
, It is prone to drug resistance, and drug resistance has become one of the main reasons for the failure of ART treatment
.
Drug resistance has become a “blocker” in achieving the three 95% anti-AIDS targets.
The World Health Organization (WHO) pointed out[2] that in some areas, HIV drug resistance has become a problem worthy of warning.
The emergence of drug viruses puts the risk of partial or complete failure of antiretroviral drugs
.
The UN’s “Political Declaration to End the AIDS Epidemic by 2030” on June 8, 2021 promised to achieve the “3 95%” target by 2030, that is, 95% of HIV-infected persons can be diagnosed, and 95% of those diagnosed can be diagnosed.
Access to ART treatment, and 95% of the patients receiving the treatment, the virus is suppressed, to achieve the goal of ending the AIDS epidemic by 2030 [3]
.
The emergence of HIV drug resistance will severely affect the virological suppression of HIV-infected persons receiving ART treatment, which will bring huge challenges to AIDS treatment and the realization of "three 95%"
.
Figure 1: The United Nations promises to achieve the "3 95%" prevention and control goals by 2030.
With the advancement of technology, there are more and more AIDS treatment options.
The compound monolithic preparation of Integrase Inhibitor (INSTI) program is BKN C Can Nuopian (B/F/TAF) be able to calmly deal with the "drug resistance crisis"? Let's take a look together
.
The B/F/TAF program has achieved long-term zero drug resistance in a number of clinical studies and played an important role in improving compliance, reducing drug resistance, and ensuring strong treatment; INSTI has strong anti-HIV activity and a better drug resistance barrier.
High, excellent virus suppression efficacy, while having both long-term safety and good tolerability
.
Clinical studies have shown that B/F/TAF is a treatment option that is not easy to develop drug resistance, whether it is in newly-treated HIV-infected patients or treated HIV-infected patients
.
The pooled results of two randomized, double-blind, controlled phase III studies 1489 and 1490 showed that [4] that newly-treated HIV-infected patients who received B/F/TAF treatment did not show any difference in follow-up for up to 4 years (192 weeks).
Treatment of related bictitgravir (BIC), emtricitabine (FTC), or propofol tenofovir (TAF) resistance mutations achieved a drug resistance outcome of 192 weeks 0
.
Table 1: Drug resistance outcome at week 192 of B/F/TAF treatment INSTI, integrase chain transfer inhibitor; NRTI, nucleoside reverse transcriptase inhibitor B/F/TAF not only achieved 192 weeks of 0 drug resistance, but also in curative effect The results of this 4-year follow-up show that at the 192th week, up to 99.
2% of B/F/TAF subjects were able to achieve virological suppression (HIV-1 RNA<50c/mL, M=E analysis)
.
Figure 2: The virological suppression of study 1489 and study 1490 at week 192 was shown in a clinical study of treated HIV-infected persons (studies 1844 and 1878) [5], HIV infection receiving B/F/TAF treatment At 116 weeks, there were no treatment-related BIC, FTC or TAF resistance mutations, and they achieved zero resistance at 116 weeks
.
The B/F/TAF program has a high resistance barrier and calmly responds to the protracted war against "AIDS".
From a mechanism point of view, the BIC in the B/F/TAF program can strongly inhibit the virus integrase, block the integration of the virus into the host DNA, and It can bind firmly to the target and has a high resistance barrier
.
The dissociation coefficient of integrase is a parameter used in drug development.
In theory, the longer the binding time, the tighter the binding, and the less likely the active ingredient of the drug will fall off the target; once it falls off, it may cause the virus to continue to replicate Or integration, resulting in drug-resistant mutations
.
The latest integrase inhibitor BIC in B/F/TAF has an innovative structure with a dissociation half-life of up to 38h[6,7]
.
Figure 3: The longest dissociation half-life of BIC and wild-type HIV-1 DNA complex, B/F/TAF, is due to its high resistance barrier.
In the in vitro tolerance test [8] compared with other containing dolutegravir ( DTG) protocol is less likely to have drug-resistant mutations, and M184I mutation occurs when the simulated missed administration of 4 doses
.
On the other hand, DTG + Lavmidine (3TC) had M184V/I and V75I resistance mutations when the simulated missed two doses were administered
.
This also shows that B/F/TAF has better tolerance for medication
.
Figure 4: Summary of the in vitro tolerance test The problem of HIV drug resistance has received more and more attention in recent years.
In the protracted battle against "AIDS", the emergence of drug resistance has undoubtedly caused a great deal of drug use for HIV-infected patients.
Trouble, greatly increasing the difficulty of treatment
.
B/F/TAF can bring strong and long-lasting virological suppression for HIV-infected people, while avoiding more drug resistance, helping HIV-infected people to quickly and effectively control the virus in the body, improve medication compliance, and calmly respond to anti-AIDS Protracted war
.
Reference materials: [1] Tang Qi, Lu Hongzhou.
The current status of AIDS epidemic and discussion on prevention and treatment strategies[J].
Fudan Journal (Medical Edition),2017,44(06):744-751.
[2]World Health Organization.
Update of recommendations on first-and second-line antiretroviral regimens.
World Health Organization (2019).
[3]Political Declaration on HIV and AIDS: Ending Inequalities and Getting on Track to End AIDS by 2030 [EB/OL].
(2021-06-09 ).
[4]Ambas J, et al.
vIAS 2021.
Poster #PEB151[5]Chloe Orkin,et al.
Long-term Efficacy and Safety of Bictegravir/Emtricitabine/Tenofovir Alafenamide in ART-Naïve Adults.
Presented at 17th European AIDS Conference, November 6–9, 2019, Basel, Switzerland[6]Lazerwith SE, et al.
ASM 2016.
Boston, MA.
Poster #414.
[7]Tsiang M, et al.
ASM 2016.
Boston, MA.
Poster # 416.
[8] Acosta RK, et al.
IDWeek 2021, Poster #888.
This information is for medical and scientific reference only.
It is not recommended to use this product in any way that is inconsistent with the prescription information approved by your country.
The problem of HIV resistance should not be underestimated! AIDS is a serious infectious disease caused by the human immunodeficiency virus (HIV), and it is one of the serious public health challenges worldwide
.
HIV takes the most important CD4+ T lymphocytes in the human immune system as the main target and conducts large-scale destruction, ultimately destroying the patient's immune function, leading to fatal opportunistic infections and malignant tumors [1]
.
In recent years, the application of anti-retroviral therapy (ART) has made AIDS a chronic and controllable disease.
However, because HIV is a retrovirus, it has a high error rate and strong variability in the process of replication and evolution.
, It is prone to drug resistance, and drug resistance has become one of the main reasons for the failure of ART treatment
.
Drug resistance has become a “blocker” in achieving the three 95% anti-AIDS targets.
The World Health Organization (WHO) pointed out[2] that in some areas, HIV drug resistance has become a problem worthy of warning.
The emergence of drug viruses puts the risk of partial or complete failure of antiretroviral drugs
.
The UN’s “Political Declaration to End the AIDS Epidemic by 2030” on June 8, 2021 promised to achieve the “3 95%” target by 2030, that is, 95% of HIV-infected persons can be diagnosed, and 95% of those diagnosed can be diagnosed.
Access to ART treatment, and 95% of the patients receiving the treatment, the virus is suppressed, to achieve the goal of ending the AIDS epidemic by 2030 [3]
.
The emergence of HIV drug resistance will severely affect the virological suppression of HIV-infected persons receiving ART treatment, which will bring huge challenges to AIDS treatment and the realization of "three 95%"
.
Figure 1: The United Nations promises to achieve the "3 95%" prevention and control goals by 2030.
With the advancement of technology, there are more and more AIDS treatment options.
The compound monolithic preparation of Integrase Inhibitor (INSTI) program is BKN C Can Nuopian (B/F/TAF) be able to calmly deal with the "drug resistance crisis"? Let's take a look together
.
The B/F/TAF program has achieved long-term zero drug resistance in a number of clinical studies and played an important role in improving compliance, reducing drug resistance, and ensuring strong treatment; INSTI has strong anti-HIV activity and a better drug resistance barrier.
High, excellent virus suppression efficacy, while having both long-term safety and good tolerability
.
Clinical studies have shown that B/F/TAF is a treatment option that is not easy to develop drug resistance, whether it is in newly-treated HIV-infected patients or treated HIV-infected patients
.
The pooled results of two randomized, double-blind, controlled phase III studies 1489 and 1490 showed that [4] that newly-treated HIV-infected patients who received B/F/TAF treatment did not show any difference in follow-up for up to 4 years (192 weeks).
Treatment of related bictitgravir (BIC), emtricitabine (FTC), or propofol tenofovir (TAF) resistance mutations achieved a drug resistance outcome of 192 weeks 0
.
Table 1: Drug resistance outcome at week 192 of B/F/TAF treatment INSTI, integrase chain transfer inhibitor; NRTI, nucleoside reverse transcriptase inhibitor B/F/TAF not only achieved 192 weeks of 0 drug resistance, but also in curative effect The results of this 4-year follow-up show that at the 192th week, up to 99.
2% of B/F/TAF subjects were able to achieve virological suppression (HIV-1 RNA<50c/mL, M=E analysis)
.
Figure 2: The virological suppression of study 1489 and study 1490 at week 192 was shown in a clinical study of treated HIV-infected persons (studies 1844 and 1878) [5], HIV infection receiving B/F/TAF treatment At 116 weeks, there were no treatment-related BIC, FTC or TAF resistance mutations, and they achieved zero resistance at 116 weeks
.
The B/F/TAF program has a high resistance barrier and calmly responds to the protracted war against "AIDS".
From a mechanism point of view, the BIC in the B/F/TAF program can strongly inhibit the virus integrase, block the integration of the virus into the host DNA, and It can bind firmly to the target and has a high resistance barrier
.
The dissociation coefficient of integrase is a parameter used in drug development.
In theory, the longer the binding time, the tighter the binding, and the less likely the active ingredient of the drug will fall off the target; once it falls off, it may cause the virus to continue to replicate Or integration, resulting in drug-resistant mutations
.
The latest integrase inhibitor BIC in B/F/TAF has an innovative structure with a dissociation half-life of up to 38h[6,7]
.
Figure 3: The longest dissociation half-life of BIC and wild-type HIV-1 DNA complex, B/F/TAF, is due to its high resistance barrier.
In the in vitro tolerance test [8] compared with other containing dolutegravir ( DTG) protocol is less likely to have drug-resistant mutations, and M184I mutation occurs when the simulated missed administration of 4 doses
.
On the other hand, DTG + Lavmidine (3TC) had M184V/I and V75I resistance mutations when the simulated missed two doses were administered
.
This also shows that B/F/TAF has better tolerance for medication
.
Figure 4: Summary of the in vitro tolerance test The problem of HIV drug resistance has received more and more attention in recent years.
In the protracted battle against "AIDS", the emergence of drug resistance has undoubtedly caused a great deal of drug use for HIV-infected patients.
Trouble, greatly increasing the difficulty of treatment
.
B/F/TAF can bring strong and long-lasting virological suppression for HIV-infected people, while avoiding more drug resistance, helping HIV-infected people to quickly and effectively control the virus in the body, improve medication compliance, and calmly respond to anti-AIDS Protracted war
.
Reference materials: [1] Tang Qi, Lu Hongzhou.
The current status of AIDS epidemic and discussion on prevention and treatment strategies[J].
Fudan Journal (Medical Edition),2017,44(06):744-751.
[2]World Health Organization.
Update of recommendations on first-and second-line antiretroviral regimens.
World Health Organization (2019).
[3]Political Declaration on HIV and AIDS: Ending Inequalities and Getting on Track to End AIDS by 2030 [EB/OL].
(2021-06-09 ).
[4]Ambas J, et al.
vIAS 2021.
Poster #PEB151[5]Chloe Orkin,et al.
Long-term Efficacy and Safety of Bictegravir/Emtricitabine/Tenofovir Alafenamide in ART-Naïve Adults.
Presented at 17th European AIDS Conference, November 6–9, 2019, Basel, Switzerland[6]Lazerwith SE, et al.
ASM 2016.
Boston, MA.
Poster #414.
[7]Tsiang M, et al.
ASM 2016.
Boston, MA.
Poster # 416.
[8] Acosta RK, et al.
IDWeek 2021, Poster #888.
This information is for medical and scientific reference only.
It is not recommended to use this product in any way that is inconsistent with the prescription information approved by your country.
