Clinical Trials

Numerous clinical trials have evaluated the therapeutic potential, safety, and pharmacological properties of Darapladib across Phase 1, Phase 2, and Phase 3 studies sponsored primarily by GlaxoSmithKline and the Mayo Clinic. These research efforts focus on cardiovascular and vascular diseases, specifically targeting atherosclerosis, endothelial dysfunction, coronary heart disease, acute coronary syndrome, and diabetic retinopathy. Completed early-phase investigations have assessed the drug's safety, pharmacokinetics, pharmacodynamics, and drug-drug interactions in human cohorts.

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01067339 COMPLETED
Endothelial Dysfunction
Mayo Clinic
 2010-02-04 PHASE3
NCT02058641 COMPLETED
Atherosclerosis
GlaxoSmithKline
 2014-02-26 PHASE1
NCT01000727 COMPLETED
Acute Coronary Syndrome
GlaxoSmithKline
 2009-12-01 PHASE3
NCT02000804 COMPLETED
Atherosclerosis
GlaxoSmithKline
 2013-10-23 PHASE1
NCT00799903 COMPLETED
Atherosclerosis
GlaxoSmithKline
 2008-12-01 PHASE3
NCT02000804 Completed
Atherosclerosis
GlaxoSmithKline
 2013-10-23 Phase 1
NCT01852565 COMPLETED
Atherosclerosis
GlaxoSmithKline
 2013-05-14 PHASE1
NCT01873339 COMPLETED
Atherosclerosis
GlaxoSmithKline
 2013-06-19 PHASE1
NCT01873339 Completed
Atherosclerosis
GlaxoSmithKline
 2013-06-19 Phase 1
NCT01852565 Completed
Atherosclerosis
GlaxoSmithKline
 2013-05-14 Phase 1
NCT01711723 COMPLETED
Atherosclerosis
GlaxoSmithKline
 2012-10-29 PHASE1
NCT01751074 COMPLETED
Atherosclerosis
GlaxoSmithKline
 2012-12-17 PHASE1
NCT01506895 COMPLETED
Retinopathy, Diabetic
GlaxoSmithKline
 2012-02 PHASE2
NCT01751074 Completed
Atherosclerosis
GlaxoSmithKline
 2012-12-17 Phase 1
NCT01711723 Completed
Atherosclerosis
GlaxoSmithKline
 2012-10-29 Phase 1
NCT01154114 COMPLETED
Atherosclerosis
GlaxoSmithKline
 2010-07-01 PHASE1
NCT01154114 Completed
Atherosclerosis
GlaxoSmithKline
 2010-07-01 Phase 1
NCT00743860 COMPLETED
Atherosclerosis
GlaxoSmithKline
 2008-09 PHASE1
NCT00704431 COMPLETED
Atherosclerosis
GlaxoSmithKline
 2008-05 PHASE1
NCT00622830 COMPLETED
Atherosclerosis
GlaxoSmithKline
 2008-01 PHASE1
NCT00551317 COMPLETED
Atherosclerosis
GlaxoSmithKline
 2007-07 PHASE1
NCT00411073 COMPLETED
Atherosclerosis
GlaxoSmithKline
 2006-12 PHASE1

(data from https://clinicaltrials.gov, updated on 2017-04-18)

Check the Darapladib (SB-480848) product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

Darapladib acts as a potent, reversible inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2) with an IC50 of 0.25 nM, effectively blocking the hydrolysis of oxidized phospholipids and preventing the generation of pro-inflammatory lysophosphatidylcholine within vascular walls. By mitigating vascular inflammatory responses and necrotic core expansion in atheromatous lesions, this targeted inhibition provides clinical relevance for managing atherosclerosis, coronary heart disease, and associated vascular dysfunctions.

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.