Clinical Trials

Several completed Phase 1 clinical trials sponsored by Pfizer and ViiV Healthcare evaluated lersivirine (UK-453061) in healthy volunteers. These early-stage investigations characterized the drug's pharmacokinetic profile, safety, tolerability, relative bioavailability, and potential drug-drug interactions with co-administered agents such as abacavir/lamivudine and rifabutin. Together, these trial data provided preliminary assessments to establish safety baselines and optimize dosing regimens prior to advanced therapeutic evaluation.

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01220232 Completed
Healthy Volunteers
Pfizer|ViiV Healthcare
 2010-11 Phase 1
NCT01230385 Completed
Healthy Volunteers
Pfizer|ViiV Healthcare
 2010-10 Phase 1
NCT00925535 Completed
Healthy Volunteers
Pfizer
 2010-05 Phase 1
NCT01050751 Completed
Healthy Volunteers
Pfizer
 2010-02 Phase 1

(data from https://clinicaltrials.gov, updated on 2024-05-22)

Check the Lersivirine (UK-453061) product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

Lersivirine functions as a non-nucleoside reverse transcriptase inhibitor (NNRTI) that selectively binds to an allosteric pocket on viral reverse transcriptase, thereby suppressing RNA-dependent DNA polymerase activity and halting retroviral replication. By blocking cDNA synthesis within host cells, this targeted enzymatic inhibition prevents viral propagation and establishes the biological basis for evaluating lersivirine safety and pharmacokinetic dynamics in healthy volunteer studies.

Appendix RUO and cGMP Quality Standards

Quality Dimension RUO (Research Use Only) cGMP (Current Good Manufacturing Practice)
Clinical Applicability Prohibited in human clinical trials or medical diagnostics. Mandatory for human clinical trials (Phase I–III) and therapies.
Regulatory Status Non-regulated grade; exempt from drug manufacturing laws. Legally enforced by health authorities (e.g., FDA, EMA, NMPA).
Facility Environment Unclassified analytical or research laboratories. Validated Cleanrooms (ISO Class 5–8) with continuous monitoring.
Quality Control Basic purity and activity testing. Rigorous safety release testing (Sterility, Endotoxin, Mycoplasma).
Process Validation Basic equipment calibration; no process validation required. Full qualification (IQ/OQ/PQ) and complete batch records.
Quality Assurance Vendor self-declared without required formal QMS. Mandatory QA/QC unit, Change Control, CAPA, and vendor audits.
Regulatory Impact High risk of IND rejection if used as a critical raw material. Required for IND/NDA filings, supported by Drug Master Files (DMF).

Footnotes

Regulatory Note: Governed by FDA (21 CFR Parts 210/211/312), EMA (EudraLex Vol 4), ICH Guidelines (E6/Q7/Q9/Q10), and compendial standards (USP <71>/<85>/<1043>).

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Note: Technical data last updated: Sep 1, 2026.