Delving into the Latest Updates on Abacavir Sulfate/Lamivudine/Zidovudine with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Abacavir (as sulfate)/Lamivudine/Zidovudine, Abacavir/lamivudine/zidovudine, Abacavir/zidovudine/lamivudine

+ [8]

Target

RT

Mechanism

RT inhibitors(Reverse transcriptase inhibitors)

Therapeutic Areas

Immune System DiseasesInfectious DiseasesUrogenital Diseases

Active Indication

HIV Infections

Inactive Indication-

Originator Organization

ViiV Healthcare Ltd.

Active Organization

ViiV Healthcare BVViiV Healthcare UK Ltd.

Inactive Organization

ViiV Healthcare Co.

Drug Highest PhaseApproved

First Approval Date

US (14 Nov 2000),

HIV Infections

RegulationAccelerated Approval (US)

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Structure/Sequence

Molecular FormulaC32H42N14O8S

InChIKeyYATVXQQJLKIPSI-SBGMWXOCSA-N

CAS Registry364057-50-1

Aicardi-Goutières syndrome (AGS) is a disease of children, particularly affecting the brain and the skin. There is a close link between AGS and increased amounts of a chemical called interferon. Normally humans only produce interferon when they are infected with a virus. In AGS, there is no viral infection. Instead, the cells in the cells of affected patients are confused into thinking that their own genetic material is coming from a virus. As a result they produce interferon all the time, which acts as a poison that damages the cells. The Investigators wish to treat AGS patients with drugs called reverse transcriptase inhibitors (RTIs), used to fight the HIV-1 virus that causes AIDS. The investigators will monitor the effect of treatment on interferon levels, and look at other markers which might give us clues to how the drugs are working. The trial is funded by the Medical Research Council, and involves experts based in Edinburgh, Birmingham, Manchester and Great Ormond Street Hospital.

Start Date24 Aug 2022

Sponsor / Collaborator

The University of Edinburgh

[+2]

NCT02363452

/ CompletedPhase 2IIT

A Pilot Clinical Trial of Reverse Transcriptase Inhibitors in Children With Aicardi-Goutières Syndrome (AGS)

The purpose of this study is to determine if treatment with reverse transcriptase inhibitors returns the interferon signature observed in patients with AGS to normal levels.

Start Date10 Sep 2015

Sponsor / Collaborator

Assistance Publique des Hôpitaux de Paris SA

NCT01352715

/ CompletedPhase 3IIT

Multicenter Study of Options for Second-Line Effective Combination Therapy (SELECT)

The study was conducted on people who were taking their first anti-HIV drug regimen (including an Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI), a type of anti-HIV drug) but the drugs in this regimen were not doing a good job of fighting their HIV infection.
The main purpose of this study was to compare two other anti-HIV drug regimens to see how well they fight HIV. The study also looked at how well participants tolerate the drug regimens and how safe they are.
The study was designed to determine whether taking the combination of lopinavir/ritonavir (LPV/r) plus raltegravir (RAL) works as well as what is usually used for second-line therapy: LPV/r plus the best-available nucleoside (nucleotide) reverse transcriptase inhibitor (NRTI) combination. Testing a regimen that does not include any NRTIs was important because NRTIs may no longer work for patients who received them as part of their first treatment regimen.

Start Date13 Mar 2012

Sponsor / Collaborator

The Aids Clinical Trials Group

[+1]

100 Clinical Results associated with Abacavir Sulfate/Lamivudine/Zidovudine

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100 Translational Medicine associated with Abacavir Sulfate/Lamivudine/Zidovudine

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100 Patents (Medical) associated with Abacavir Sulfate/Lamivudine/Zidovudine

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42

Literatures (Medical) associated with Abacavir Sulfate/Lamivudine/Zidovudine

01 Apr 2014·HIV Clinical Trials

Switching to an Etravirine-Containing Regimen Due to Drug Intolerance in Clinical Practice

Article

Author: Moreno, V ; Ramírez-Olivenza, G ; Martín-Carbonero, L ; Valencia, E

BACKGROUNDDrug intolerance is one of the main reasons for switching antiretroviral therapy in HIV-infected patients. Etravirine (ETR) has demonstrated good tolerability in clinical trials and may be an option for patients who switch therapy due to adverse events.METHODSWe retrospectively reviewed all patients who had switched to an ETR-containing regimen in our center due to side effects. Virological suppression, ETR discontinuation, and reasons for discontinuation were studied.RESULTSA total of 78 patients started treatment with ETR in our center due to previous regimen toxicity. Most of them were men (83.3%), and the median time of infection was 14 years (IQR, 6.5-20 years). HIV RNA was <35 copies/mL in 88.3% of patients, although 33% had archived non-nucleos(t)ide reverse transcriptase inhibitor (NNRTI) mutations that did not compromise ETR efficacy. Efavirenz was the drug most often replaced (38.5%), followed by atazanavir (20.5%) and lopinavir (6.4%). The fixed combination of Trizivir was changed in another 10.3% of patients. After a median follow-up of 14 months (IQR, 6-23), the rate of virologic suppression was 79.5% and 98.4% in intention-to-treat and on-treatment analysis, respectively. Seven patients discontinued treatment due to adverse events (3 gastrointestinal disturbances, 2 rashes, 1 swelling, and 1 neuropathy). ETR was combined with 2 nucleos(t)ide analogues in 75.4% of patients.CONCLUSIONIn HIV patients who report drug side effects, switching to an ETR-containing regimen is a safe strategy in terms of virological suppression and toxicity.

01 Apr 2014·Hearing ResearchQ1 · MEDICINE

In vitro assessment of antiretroviral drugs demonstrates potential for ototoxicity

Q1 · MEDICINE

Article

Author: Thein, Pru ; Kalinec, Gilda M ; Kalinec, Federico ; Park, Channy

Several studies have reported an increased incidence of auditory dysfunction among HIV/AIDS patients. We used auditory HEI-OC1 cells in cell viability, flow cytometry and caspases 3/7-activation studies to investigate the potential ototoxicity of fourteen HIV antiretroviral agents: Abacavir, AZT, Delavirdine, Didenosine, Efavirenz, Emtricitabine, Indinavir, Lamivudine, Nefinavir, Nevirapine, Tenofovir, Ritonavir, Stavudine and Zalcitabine, as well as combinations of these agents as used in the common anti-HIV cocktails Atripla™, Combivir™, Epzicom™, Trizivir™, and Truvada™. Our results suggested that most of the single assayed anti-HIV drugs are toxic for HEI-OC1 auditory cells. The cocktails, on the other hand, decreased auditory cells' viability with high significance, with the following severity gradient: Epzicom ∼ Trizivir >> Atripla ∼ Combivir > Truvada. Interestingly, our results suggest that Trizivir- and Epzicom-induced cell death would be mediated by a caspase-independent mechanism. l-Carnitine, a natural micronutrient known to protect HEI-OC1 cells against some ototoxic drugs as well as to decrease neuropathies associated with anti-HIV treatments, increased viability of cells treated with Lamivudine and Tenofovir as well as with the cocktail Atripla, but had only minor effects on cells treated with other drugs and drug combinations. Altogether, these results suggest that some frequently used anti-HIV agents could have deleterious effects on patients' hearing, and provide arguments in favor of additional studies aimed at elucidating the potential ototoxicity of current as well as future anti-HIV drugs.

01 Apr 2012·Journal of the International AIDS SocietyQ2 · MEDICINE

Abacavir alters the transcription of inflammatory cytokines in virologically suppressed, HIV‐infected women

Q2 · MEDICINE

ArticleOA

Author: Lockman, Shahin ; Ogwu, Anthony ; Rowley, Christopher F. ; Mmalane, Mompati ; MacLeod, Iain J. ; Moyo, Sikhulile ; Essex, M. ; van Widenfelt, Erik ; Shapiro, Roger L. ; Makhema, Joseph

BackgroundAbacavir (ABC) may be associated with a small, increased risk of myocardial infarction in HIV‐infected adults, possibly related to cytokine‐mediated inflammation.MethodsTo evaluate the induction of inflammatory cytokine transcription by ABC, we used samples from women randomized to receive zidovudine/lamivudine/ABC (Trizivir) or lopinavir/ritonavir and zidovudine/lamividine (Kaletra/Combivir) from the third trimester through six‐months postpartum for the prevention of mother‐to‐child transmission (PMTCT). Women were matched by CD4 count and baseline HIV RNA. All women attained viral suppression (<50 copies/ml) by the time of sampling.ResultsFour cytokines showed a difference in expression between the treatment arms, all in a proinflammatory direction for the ABC arm: CD40LG 1.82‐fold, (p=.027); IL‐8 3.16‐fold (p=.020); LTA 2.82‐fold, (p=.008); and CCL5 −1.67‐fold, (p=.035). At 12‐months postpartum, 6‐months after antiretroviral discontinuation, cytokine expression was similar by treatment arm.ConclusionsWe conclude that ABC may upregulate proinflammatory cytokines at the transcriptional level in this population.

100 Deals associated with Abacavir Sulfate/Lamivudine/Zidovudine

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External Link

KEGG	Wiki	ATC	Drug Bank
-	Abacavir Sulfate/Lamivudine/Zidovudine	J05AR04	-

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
HIV Infections	LI	ViiV Healthcare BV	27 Dec 2000
HIV Infections	EU	ViiV Healthcare BV	27 Dec 2000
HIV Infections	IS	ViiV Healthcare BV	27 Dec 2000
HIV Infections	NO	ViiV Healthcare BV	27 Dec 2000

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT01352715 (A5273 \| SELECT, CTgov)	Phase 3	HIV Infections	515	Lopinavir/ritonavir+raltegravir (Arm A: LPV/r Plus RAL)	bcmwoymthe(imjsrktmec) = juwifpvcac strdtrgpvm (njqcqdqjqk, yyawzmauam - fglccmsyxm) View more	-	06 Jan 2016
				Abacavir/lamivudine+Zidovudine+Abacavir+Lamivudine/zidovudine+Abacavir/lamivudine/zidovudine+Emtricitabine/tenofovir disoproxil fumarate+Lamivudine+Lopinavir/ritonavir (Arm B: LPV/r Plus Best Available NRTIs)	bcmwoymthe(imjsrktmec) = nhfaqwonea strdtrgpvm (njqcqdqjqk, prjcdyoxcm - yspqqwxflg) View more
NCT00851630 (THIRST, CTgov)	Phase 4	Tuberculosis \| HIV Infections \| Immune Reconstitution Inflammatory Syndrome	70	Fixed dose combination zidovudine/lamivudine/abacavir (Early)	qvemvjjvlf(gkrxbgzwlz) = xzmyljoplc syenwglous (liwoiqerqo, rwztqnessy - oiawvkfbdw) View more	-	08 Jan 2010
				Fixed dose combination zidovudine/lamivudine/abacavir (Delayed)	qvemvjjvlf(gkrxbgzwlz) = fejzfzdvnb syenwglous (liwoiqerqo, slewippjap - csfskkmrtx) View more
IAS2010	Not Applicable	AIDS-related Kaposi Sarcoma	23	Co-formulated abacavir/lamivudine/zidovudine	okrgtvxntg(mqmnaubasy) = xogvlgzyel tcjdqjxugt (ydfmvmqkvy )	-	01 Jan 2010
				Co-formulated abacavir/lamivudine plus co-formulated lopinavir/ritonavir	okrgtvxntg(mqmnaubasy) = kjjbqghvde tcjdqjxugt (ydfmvmqkvy )
COL40275 (IAS2007)	Not Applicable	Hepatitis B, Chronic \| HIV Infections	9	Abacavir/Zidovudine/Lamivudine + Tenofovir	vlqjbusgat(iubtanjlcu) = twllcmewem kqqfzeegjq (xmloxvtonh )	-	01 Jan 2007
IAS2007	Not Applicable	HIV Infections	54	Trizivir (TZV) plus tenofovir (TDF)	(fcawtptdje) = mxmuuzujta bbtrpbpmtt (mjqxgvukpv ) View more	-	01 Jan 2007
COL40193 (IAS2006)	Not Applicable	Maintenance	23	Trizivir/Kaletra	(zppbnfucaf) = Drug-related AEs occurred in 13/23 subjects, with gastrointestinal disorders the most common (10/23) xokwyezglz (cpguzncomo ) View more	-	01 Jan 2006
				Trizivir
IAS2006	Not Applicable	Kaposi Sarcoma	90	Co-formulated abacavir/lamivudine/zidovudine	gvsufofpwb(voxywbghpk) = uncommon (1%) jbnclzmtgu (knabtmcxfw )	-	01 Jan 2006
IAS2006	Not Applicable	HIV Infections	155	Trizivir-containing combination of antiretrovirals	(luxbjbgiyp) = ydwpdopadl qotzauipww (wawighgiey, 99 - 370) View more	-	01 Jan 2006
IAS2006	Not Applicable	-	54	Trizivir + TDF	rpqdbalvjz(cpntoswcar) = ycrrerkhyw locwoholuu (tizcyoogan ) View more	-	01 Jan 2006
IAS2005	Not Applicable	Hypersensitivity \| Drug-Related Side Effects and Adverse Reactions	-	Ziagen	gnpbgmxzzh(ophyxwjwjr) = hjznusivjj ftdnolxial (qnmosyeigy ) View more	-	01 Jan 2005
				Trizivir	gnpbgmxzzh(ophyxwjwjr) = lnkjrsuvhy ftdnolxial (qnmosyeigy ) View more