Delving into the Latest Updates on Lersivirine with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Lersivirine (USAN/INN)

Target

RT

Mechanism

RT inhibitors(Reverse transcriptase inhibitors)

Therapeutic Areas

Immune System DiseasesInfectious DiseasesUrogenital Diseases

Active Indication-

Inactive Indication

HIV Infections

Originator Organization

Pfizer Inc.

Active Organization-

Inactive Organization

Pfizer Inc.

ViiV Healthcare Ltd.

Drug Highest PhaseDiscontinuedPhase 2

First Approval Date-

Regulation-

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Structure

Molecular FormulaC17H18N4O2

InChIKeyMCPUZZJBAHRIPO-UHFFFAOYSA-N

CAS Registry473921-12-9

The purpose of this study is to estimate the pharmacokinetics (PK) of 3 different modified-release formulations of lersivirine and compare it to the PK of the immediate-release tablet. The effect of food on the PK of one of the modified-release tablets will also be assess along with the safety and tolerability of each treatment.

Start Date01 Jun 2012

Sponsor / Collaborator

Pfizer Inc.

[+1]

EUCTR2010-020860-39-IT / Not yet recruitingNot Applicable

A LONG-TERM OPEN-LABEL EXTENSION STUDY OF LERSIVIRINE FOR THE TREATMENT OF HIV-1 INFECTION - ND

Start Date05 Feb 2011

Sponsor / Collaborator

Pfizer Inc.

NCT01254656 / TerminatedPhase 2

A Long Term Open-Label Extension Study Of Lersivirine For The Treatment Of HIV-1 Infection

This is a study to assess long-term safety and efficacy of lersivirine in patients who have completed 96 weeks of treatment with lersivirine in studies A5271015 and A5271022.

Start Date01 Feb 2011

Sponsor / Collaborator

Pfizer Inc.

[+1]

100 Clinical Results associated with Lersivirine

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100 Translational Medicine associated with Lersivirine

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100 Patents (Medical) associated with Lersivirine

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32

Literatures (Medical) associated with Lersivirine

01 Apr 2015·Toxicologic PathologyQ4 · MEDICINE

Two-year Carcinogenicity Study in Rats with a Nonnucleoside Reverse Transcriptase Inhibitor

Q4 · MEDICINE

Article

Author: Nambiar, Prashant R. ; Bailey, Steven A. ; Houle, Christopher ; Morton, Daniel ; Finch, Gregory L. ; Dochterman, Leland Wayne ; Thomford, Peter J. ; Fate, Gwendolyn

Administration of lersivirine, a nonnucleotide reverse transcriptase inhibitor, daily by oral gavage to Sprague-Dawley rats for up to 2 yr was associated with decreased survival, decreased body weights, and an increase in neoplasms and related proliferative lesions in the liver, thyroid, kidney, and urinary bladder. Thyroid follicular adenoma and carcinoma, the associated thyroid follicular hypertrophy/hyperplasia, hepatocellular adenoma/adenocarcinoma, altered cell foci, and hepatocellular hypertrophy were consistent with lersivirine-related induction of hepatic microsomal enzymes. Renal tubular adenoma and renal tubular hyperplasia were attributed to the lersivirine-related exacerbation of chronic progressive nephropathy (CPN), while urinary bladder hyperplasia and transitional cell carcinoma in the renal pelvis and urinary bladder were attributed to urinary calculi. Renal tubular neoplasms associated with increased incidence and severity of CPN, neoplasms of transitional epithelium attributed to crystalluria, and thyroid follicular and hepatocellular neoplasms related to hepatic enzyme induction have low relevance for human risk assessment.

16 Jan 2015·Organic LettersQ1 · CHEMISTRY

Mild Palladium-Catalyzed Cyanation of (Hetero)aryl Halides and Triflates in Aqueous Media

Q1 · CHEMISTRY

Article

Author: Cohen, Daniel T. ; Buchwald, Stephen L.

A mild, efficient, and low-temperature palladium-catalyzed cyanation of (hetero)aryl halides and triflates is reported. Previous palladium-catalyzed cyanations of (hetero)aryl halides have required higher temperatures to achieve good catalytic activity. This current reaction allows the cyanation of a general scope of (hetero)aryl halides and triflates at 2-5 mol % catalyst loadings with temperatures ranging from rt to 40 °C. This mild method was applied to the synthesis of lersivirine, a reverse transcriptase inhibitor.

01 Nov 2014·Clinical Pharmacology in Drug Development

Single‐dose pharmacokinetics, safety, and tolerability of modified‐release formulations of lersivirine in healthy subjects

Article

Author: Wang, Cunshan ; Heera, Jayvant ; Mukwaya, Geoffrey ; Wang, Ronnie ; Weatherley, Barry ; Vourvahis, Manoli ; Tawadrous, Margaret ; Mendes da Costa, Laure

This article identifies a MR lersivirine formulation with a lower C_max than the IR formulation but with comparable total plasma exposures (AUC).Modified-release (MR) lersivirine was associated with good tolerability among the small number of healthy subjects were discussed in this article.

100 Deals associated with Lersivirine

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External Link

KEGG	Wiki	ATC	Drug Bank
D09634	Lersivirine	-	DB11649

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
HIV Infections	Phase 2	DE	ViiV Healthcare Ltd.	01 Feb 2006
HIV Infections	Phase 2	DE	ViiV Healthcare Ltd.	01 Feb 2006
HIV Infections	Phase 2	DE	Pfizer Inc.	01 Feb 2006
HIV Infections	Phase 2	DE	Pfizer Inc.	01 Feb 2006

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT00823979 (CTgov)	Phase 2	HIV Infections	105	Lersivirine (Lersivirine 750 mg)	otnxtddqop(neynurzpmj) = ppnmkduzjt tjpdjswxyp (ycplrxxenk, anqytfrikr - iiirmuqqul) View more	-	14 Mar 2014
				Lersivirine (Lersivirine 1000 mg)	otnxtddqop(neynurzpmj) = ammrhjzthv tjpdjswxyp (ycplrxxenk, krtfjzmcru - ffckgwgvzs) View more
NCT00824421 (CTgov)	Phase 2	HIV Infections	195	Lersivirine (Lersivirine 500 mg)	uwgkqsdwyb(npefrycfqr) = mxmxpxhigu fejztzmryz (lsaecoadfk, jldaqwzoth - uclsmazids) View more	-	24 Jan 2014
				Lersivirine (Lersivirine 750 mg)	uwgkqsdwyb(npefrycfqr) = sanwitzykd fejztzmryz (lsaecoadfk, jxjaqnsyzc - iddpepzqsn) View more
NCT00348673 (CTgov)	Phase 2	HIV Infections	49	UK-453,061 (UK-453,061 10 mg Twice Daily (Stage 1))	nkewhqdzyh(crhhjqrygf) = ertoqtzksf zdksfpxptn (vcdumqflxx, nepgqaopfa - qontpdvtoc) View more	-	18 Oct 2013
				UK-453,061 (UK-453,061 30 mg Twice Daily (Stage 1))	nkewhqdzyh(crhhjqrygf) = hxtajpwqqc zdksfpxptn (vcdumqflxx, bfbhwchbsx - qxkuvdigrm) View more
A5271015 (IAS2011)	Not Applicable	-	128	Lersivirine (500/750 mg QD)	(bqgbupgukm) = zjhclgmapf yfqhethzna (rpknzkzbtt )	-	01 Jan 2011
A5271015 (IAS2011)	Not Applicable	-	193	Lersivirine 500mg	hcviwlyfph(vgwsrbnvch) = wrtqfyczaw uwzmurzdkn (dxbkhdtxll ) View more	-	01 Jan 2011
				Lersivirine 750mg	hcviwlyfph(vgwsrbnvch) = jdifmncrbe uwzmurzdkn (dxbkhdtxll ) View more
IAS2011	Not Applicable	-	13	Lersivirine	(xjhcvhdcup) = vzdhylttze rgiteosiko (jmumlytnxv, 0.90 - 1.12) View more	-	01 Jan 2011
				Methadone	(xjhcvhdcup) = eovayeqrts rgiteosiko (jmumlytnxv, 0.85 - 1.11) View more
IAS2009	Not Applicable	HIV Infections	42	Lersivirine 10mg BID	(oyfxczfcar) = kanepmekue xpzhkijvoh (esrofpslog, 18.8%)	-	01 Jan 2009
				Lersivirine 30mg BID	(oyfxczfcar) = qhgyffnfas xpzhkijvoh (esrofpslog, 18.8%)
IAS2007	Not Applicable	-	-	UK-453,061	ctolcgxuoc(evtszceyhr) = prpbpsnqlk ytrggzwesu (zoksweywvo ) View more	-	01 Jan 2007