1. Anti-infection
    Anti-infection
  2. HIV
    Reverse Transcriptase

Lersivirine (Synonyms: UK-453061; UK453061; UK 453061)

Cat. No.: HY-14267 Purity: 96.00%
Data Sheet SDS Handling Instructions

Lersivirine(UK-453061) is a next-generation non-nucleoside reverse transcriptase inhibitor (NNRTI, IC50=119 nM) with a unique resistance profile that exhibits potent antiretroviral activity against wild-type human immunodeficiency virus and clinically relevant NNRTI-resistant strains.

For research use only. We do not sell to patients.
Lersivirine Chemical Structure

Lersivirine Chemical Structure

CAS No. : 473921-12-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO $132 In-stock
5 mg $120 In-stock
10 mg $200 In-stock
50 mg $700 In-stock
100 mg $1200 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Lersivirine(UK-453061) is a next-generation non-nucleoside reverse transcriptase inhibitor (NNRTI, IC50=119 nM) with a unique resistance profile that exhibits potent antiretroviral activity against wild-type human immunodeficiency virus and clinically relevant NNRTI-resistant strains. IC50 value: 0.119 uM [1] Target: NNRTI UK-453061(Compound 5) demonstrated excellent activity against large panels of wild type and drug-resistant HIV consistent with the encouraging profile demonstrated against the isolated RT enzymes. Compound 5 can be readily prepared in multi-gram quantities by virtue of the efficient and concise synthetic route. The compound also has good aqueous solubility and formulation characteristics which enable further in vivo evaluation. Clinical trials evaluating the potential of 5 (UK-453,061, lersivirine) to treat HIV infection are proceeding and further progress will be reported in due course [1]. At clinically relevant lersivirine doses (500-1,000 mg total daily dose), the mean plasma exposure of midazolam was reduced in a dose-dependent manner by 20-36 %. Co-administration of lersivirine 1,000 mg QD with OCs had minor PK effects, increasing ethinylestradiol exposure by 10 % and reducing levonorgestrel exposure by 13 % [2]. Mated Crl:CD1(ICR) mice were administered 0, 150, 350, and 500 mg/kg lersivirine once daily by oral gavage on gestation days 6 to 17, followed by cesarean section on gestation day 18. The first 2 days of dosing for the high-dose group were done at 250 mg/kg to allow induction of hepatic metabolizing enzymes, after which the dose was increased to 500 mg/kg/day [3].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT00784420 Pfizer Healthy Volunteers September 2008 Phase 1
NCT01050751 Pfizer Healthy Volunteers February 2010 Phase 1
NCT00823979 Pfizer HIV-1 March 2009 Phase 2
NCT00936871 Pfizer Healthy Volunteers January 2010 Phase 1
NCT00348673 Pfizer|ViiV Healthcare HIV-1 February 2006 Phase 2
NCT00925535 Pfizer Healthy Volunteers May 2010 Phase 1
NCT01603485 Pfizer|ViiV Healthcare Healthy Volunteer June 2012 Phase 1
NCT01220232 Pfizer|ViiV Healthcare Healthy Volunteers November 2010 Phase 1
NCT01099748 Pfizer Healthy Volunteers May 2010 Phase 1
NCT01230385 Pfizer|ViiV Healthcare Healthy Volunteers October 2010 Phase 1
NCT00824421 Pfizer HIV-1 February 2009 Phase 2
NCT00824369 Pfizer|ViiV Healthcare HIV-1 July 2009 Phase 2
NCT01254656 Pfizer|ViiV Healthcare HIV-1 February 2011 Phase 2
View MoreCollapse
References
M.Wt

310.35

Formula

C₁₇H₁₈N₄O₂

CAS No.

473921-12-9

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number

 

Organization name *

Country *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Lersivirine
Cat. No.:
HY-14267
Quantity: