Drugs / Darapladib
last change Nov 2015 re-read 2 minutes ago

Darapladib

also known as SB-480848

Small molecule targets PLA2G7 via inhibition

Developed for
atherosclerosis · acute coronary syndrome · diabetic macular edema
Investigated by
GlaxoSmithKline · Mayo Clinic · National Heart, Lung, and Blood Institute (NHLBI) · National Institute on Aging (NIA) · The TIMI Study Group

Trials 21 · a red edge is where a trial was stopped

PhaseRegistry idDatesIndicationSponsorStatusOutcome
Phase 113 trials
Phase 1 NCT02058641 Feb → Aug 2014 atherosclerosis GlaxoSmithKline Completed No outcome recorded
Phase 1 NCT02000804 Oct 2013 → Jan 2014 atherosclerosis GlaxoSmithKline Completed No outcome recorded
Phase 1 NCT01873339 Jun → Sep 2013 atherosclerosis GlaxoSmithKline Completed No outcome recorded
Phase 1 NCT01852565 May → Sep 2013 atherosclerosis GlaxoSmithKline Completed No outcome recorded
Phase 1 NCT01751074 Dec 2012 → Mar 2013 atherosclerosis GlaxoSmithKline Completed No outcome recorded
Phase 1 NCT01711723 Oct 2012 → Mar 2013 atherosclerosis GlaxoSmithKline Completed No outcome recorded
Phase 1 NCT01154114 Jul → Oct 2010 atherosclerosis GlaxoSmithKline Completed No outcome recorded
Phase 1 NCT00743860 Sep → Dec 2008 atherosclerosis GlaxoSmithKline Completed No outcome recorded
Phase 1 NCT00704431 May → Oct 2008 atherosclerosis GlaxoSmithKline Completed No outcome recorded
Phase 1 NCT00622830 Jan → Mar 2008 atherosclerosis GlaxoSmithKline Completed No outcome recorded
Phase 25 trials
Phase 2 NCT01506895 Feb 2012 → Feb 2013 diabetic macular edema GlaxoSmithKline Completed No outcome recorded
Phase 2 NCT00734032 Aug 2008 → Jan 2009 atherosclerosis GlaxoSmithKline Completed No outcome recorded
Phase 2 NCT00268996 Nov 2005 → Aug 2007 atherosclerosis GlaxoSmithKline Completed No outcome recorded
Phase 2 NCT00269048 Nov 2005 → Sep 2006 atherosclerosis GlaxoSmithKline Completed No outcome recorded
Phase 2 NCT01916720 Jan → Jul 2003 atherosclerosis GlaxoSmithKline Completed No outcome recorded
Phase 33 trials
Phase 3 NCT01067339 Feb 2010 → Nov 2015 Mayo Clinic Completed No outcome recorded
Phase 3 NCT01000727 Dec 2009 → Apr 2014 acute coronary syndrome GlaxoSmithKline Completed No outcome recorded
Phase 3 NCT00799903 Dec 2008 → Oct 2013 atherosclerosis GlaxoSmithKline Completed No outcome recorded

Evidence & citations 6 cited values

Every value below carries the sentence it was read from. 23 sources stand behind the page.

FieldValueCited text
Known as Darapladib “BACKGROUND: The aim of this study was to assess the effects of darapladib, a selective oral investigational lipoprotein-associated phospholipase A2 inhibitor, on both plasma...” PMID 24586490 Feb 2014
17

“This study examined the effects of darapladib, a selective lipoprotein-associated phospholipase A(2) (Lp-PLA(2)) inhibitor, on biomarkers of cardiovascular (CV) risk.” PMID 18436114 Apr 2008

“SB-480848 (Darapladib)” NCT00622830

NCT00799903

NCT01067339

NCT01000727

NCT01506895

NCT00411073

NCT00551317

NCT00704431

NCT01852565

NCT01751074

NCT01873339

NCT02058641

NCT01711723

NCT02000804

NCT01154114

NCT00743860

Known as SB-480848 “Darapladib (SB-480848) is a novel, selective, orally active inhibitor of lipoprotein associated phospholipase A2 (Lp-PLA2) currently under clinical development by...” NCT01852565
13

SB-480848 (darapladib) is a novel selective and orally active inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2) being developed by GlaxoSmithKline (GSK) for the...” NCT02000804

“A Study to Evaluate the Pharmacokinetics of the Enteric-Coated Micronized Free Base Formulation of Darapladib [SB-480848] and Its Metabolites in Healthy Volunteers.” NCT00743860

“Study to Determine the Effect of 14 Days Dosing With Darapladib (SB-480848) on Carotid Plague Composition in Patients With Planned Carotid Endarterectomy” NCT01916720

“A Study to Assess the Pharmacokinetics, Safety and Tolerability of Repeat Oral Doses of Darapladib (SB-480848) in Subjects With Severe Renal Impairment” NCT01711723

“An Open-label, Single-sequence Study to Evaluate the Potential CYP 3A4 Pharmacokinetic Interaction of Darapladib (SB-480848) in Healthy Subjects” NCT01873339

“The subjects will be administered 40 mg oral doses of darapladib (SB-480848) enteric-coated tablets daily for 10 consecutive days.” NCT01154114

“Study Of The Effects Of SB 480848 (Darapladib) On The Electrical Conduction Of The Heart” NCT00411073

SB-480848 (darapladib)” NCT00704431

“Darapladib (SB480848)” NCT00551317

NCT00368576

NCT00268996

NCT00734032

NCT00622830

Action Inhibit “Novel Lipoprotein-associated Phospholipase A2 (Lp-PLA2) Inhibitor SB-480848” NCT00268996
1

“LDL-associated phospholipase A2 inhibitor” CHEMBL204021

Modality Small molecule CHEMBL204021
Route Oral “Coronary heart disease (CHD) and CHD-risk equivalent patients (n = 959) receiving atorvastatin (20 or 80 mg) were randomized to oral darapladib 40 mg, 80 mg, 160 mg, or placebo...” PMID 18436114 Apr 2008
Target PLA2G7 “LDL-associated phospholipase A2 inhibitor” CHEMBL204021