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LOSMAPIMOD

Phase 2

Atherosclerosis | Small molecule | Cardiovascular |GSK plc|Last Updated: Oct 17, 2018

Success Probability

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Trial Design

RandomizedDouble-BlindPLACEBO_CONTROLLED
Total Trials1
Total Enrollment99

FDA Designations

No designations recorded

Clinical trial landscape

LOSMAPIMOD · 7 trials · 5 indications

Phase 2 4Phase 1 3
NCT02299375Safety and Efficacy Study of Losmapimod (GW856553) in Frequently Exacerbating Participants With Chronic Obstructive Pulmonary Disease (COPD)Pulmonary Disease, Chronic Obstructive
COMPLETED184 Analytics
NCT02000440A Phase II, Repeat Dose, Proof of Mechanism Study of Losmapimod to Reduce Proteinuria in Patients With Focal Segmental Glomerulosclerosis (FSGS)Glomerulosclerosis, Focal Segmental
COMPLETED17 Analytics
NCT01218126Randomised, Double-Blind, Placebo-Controlled, Parallel-Group, Multi-centre, Dose Ranging Study to Evaluate the Efficacy and Safety of Losmapimod Tablets Administered Twice Daily Compared With Placebo for 24 Weeks in Adult Subjects With Chronic Obstructive Pulmonary Disease (COPD).Pulmonary Disease, Chronic Obstructive
COMPLETED604 Analytics
NCT00633022A Study to Evaluate the Effects of 3 Months Dosing With GW856553, as Assessed FDG-PET/CT ImagingAtherosclerosis
COMPLETED99 Analytics
PHASE2COMPLETED
Safety and Efficacy Study of Losmapimod (GW856553) in Frequently Exacerbating Participants With Chronic Obstructive Pulmonary Disease (COPD)
Pulmonary Disease, Chronic ObstructiveUnlock trial analytics
PHASE2COMPLETED
A Phase II, Repeat Dose, Proof of Mechanism Study of Losmapimod to Reduce Proteinuria in Patients With Focal Segmental Glomerulosclerosis (FSGS)
Glomerulosclerosis, Focal SegmentalUnlock trial analytics
PHASE2COMPLETED
Randomised, Double-Blind, Placebo-Controlled, Parallel-Group, Multi-centre, Dose Ranging Study to Evaluate the Efficacy and Safety of Losmapimod Tablets Administered Twice Daily Compared With Placebo for 24 Weeks in Adult Subjects With Chronic Obstructive Pulmonary Disease (COPD).
Pulmonary Disease, Chronic ObstructiveUnlock trial analytics
PHASE2COMPLETED
A Study to Evaluate the Effects of 3 Months Dosing With GW856553, as Assessed FDG-PET/CT Imaging
AtherosclerosisUnlock trial analytics

Study Endpoints

Primary Endpoints

Annual Rate of Moderate and Severe Exacerbations of COPD
From the start of the study treatment up to 53 Weeks

An exacerbation of COPD, is defined as the worsening of 2 or more major symptoms (dyspnea, sputum volume, sputum purulence) or the worsening of any 1 major symptom together with any 1 of the minor symptoms (sore throat, cold, fever without other cause, increased cough and wheeze), for at least 2 consecutive days. Moderate-severe exacerbations were defined as use of antibiotics and/or oral steroids and/or hospitalization. Summary only included exacerbations for which a date of resolution or death was provided. Analysis was performed by using Bayesian inference assuming non-informative priors. The mean exacerbation rate was adjusted for treatment group, smoking status, ICS use and region. The adjusted posterior median was summarized per treatment group. The number of exacerbation events per participant was assumed to follow a negative binomial distribution. Modified Intent-to-Treat (mITT) Population comprised of all randomized par. who received at least one dose of study treatment.

Number of Participants Meeting the Definition of Responder for Reduction in Proteinuria at the Indicated Time Points
Week 2, Week 4, Week 8, Week 16 and Week 24

Proteinuria is defined as the presence of an excess of serum proteins in the urine. Participant was considered as a responder on achieving \>=50 percent reduction in proteinuria from Baseline (measured as 24 hour total protein) and also having a stable renal function of \>=70 percent of Baseline estimated glomerular filtration rate (eGFR) at end of treatment (\>=16 Weeks). Only those participants available at the specified time points (represented by n=X in the category titles) were analyzed.

Change From Baseline in Six Minute Walk Distance (6MWD) at Week 4, 12 and 24
Baseline (Week 0) and Week 4, 12, 24

Exercise tolerance was assessed using the 6MWD. If a participant was recorded as having used supplemental oxygen or a walking aid (including sitting down then continuing walking) or a technical problem during a 6MWD then that walk was considered as invalid; otherwise the 6MWD was considered as valid. The baseline 6MWD value was defined as the longest distance walked, for a valid walk, at Visit 2. Variability between the distances walked during the first six-minute walk test (6MWD1) and the second six-minute walk test (6MWD2) being compared was defined as: Variability = \[100 x (6MWD2 - 6MWD1)\]/6MWD1. Change from Baseline was calculated as the endpoint value minus the Baseline value. Baseline visit was Visit 2 (Week 0).

Change From Baseline of Mean of Maximum Tissue to Background Ratio (TBR) in the Qualifying Artery, Following 12 Weeks of Treatment in the Setting of Chronic Statin Therapy
Baseline (Days -14 to -1) and up to Week 12

Qualifying artery was defined as the artery (left or right carotid or ascending aorta) with the highest segmental mean of maximum (max) TBR at Baseline. The TBR of the qualifying segment was to be ≥ 1.6. If more than one artery qualified, the hottest (greatest mean of max TBR) artery was the qualifying artery. Baseline was defined as the value between Days -14 to -1. The change from Baseline was calculated by subtracting the Baseline values from the individual post-treatment values.

Change from baseline in QT interval corrected for heart rate by Fridericia's formula (QTcF) at each time point for losmapimod 20 mg QD on Day 5 as compared with time matched placebo
Baseline and Day 5 of the corresponding study period

Triplicate ECGs will be collected at three baseline pre-dose time points (at -45 min, -30 min and -15 min) on Day 1 of the corresponding study period. Period baseline will be the average of triplicate pre-dose assessments. Triplicate Holter ECGs measurements will be evaluated at 14 post-dose time points (0, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 18 and 24 hours) on Day 5 of the corresponding study period and will be averaged prior to calculation of changes from period baseline and statistical analyses

Adverse events
Single dose: up to 96h post dose. Repeat dose: up to 17 days post dose.

Number of participants with adverse events as a measure of safety and tolerability (evaluated by the result of Clinical safety laboratory tests, vital signs and 12-lead ECG).

AUC(0-t)
up to 96h post dose.

Area under the concentration-time curve from pre-dose to last time of quantifiable concentration of losmapimod and GSK198602 (inactive metabolite) (Single dose only).

AUC(0-inf)
up to 96h post dose.

Area under the concentration-time curve from time pre-dose extrapolated to infinite time of losmapimod and GSK198602 (Single dose only).

AUC(0-tau)
up to 17 days post dose.

Area under the concentration-time curve over the dosing interval of losmapimod and GSK198602 (Repeat dose only).

Cmax
Single dose: up to 96h post dose. Repeat dose: up to 17 days post dose.

Maximum observed concentration of losmapimod and GSK198602.

tmax
Single dose: up to 96h post dose. Repeat dose: up to 17 days post dose.

Time of occurrence of Cmax of losmapimod and GSK198602.

t1/2
Single dose: up to 96h post dose. Repeat dose: up to 17 days post dose.

Terminal phase half-life of losmapimod and GSK198602

accumulation ratios
up to 17 days post dose.

accumulation ratios of losmapimod and GSK198602 (Repeat dose only).

General safety and tolerability endpoints include changes in clinical laboratory assessments, spontaneous AE reporting, ECGs, vital signs and nursing/physician observations.
Up to 15 days post IV infusion.

Secondary Endpoints

Time to First Occurrence of Moderate or Severe COPD Exacerbation
From the start of the study treatment up to 53 Weeks
Number of Participants Having Any Adverse Events (AEs), Serious Adverse Events (SAEs)
From the start of the study treatment up to 53 Weeks
Change From Baseline in Spirometry Parameters in Pre and Post Forced Expiratory Volume in 1 Second (FEV1); Pre and Post Forced Vital Capacity (FVC); Pre and Post Forced Expiratory Volume in 6 Seconds (FEV6).
Baseline and up to Week 52
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Study Design & Arms

AllocationRANDOMIZED
MaskingDOUBLE
ModelPARALLEL
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
Losmapimod 15 mgEXPERIMENTALSubjects with COPD will receive losmapimod 15 mg tablets orally, twice daily, approximately 12 hours apart and within 30 minutes after meals with a full glass of water for the duration of the treatment period in addition to standard of care, stratified according to whether a center collects sputum or not and current use of inhaled corticosteroid (ICS). Salbutamol metered dose inhaler (MDI) will be provided as a rescue medication.
PlaceboEXPERIMENTALSubjects with COPD will receive placebo orally, twice daily, approximately 12 hours apart and within 30 minutes after meals with a full glass of water for the duration of the treatment period in addition to standard of care, stratified according to whether a center collects sputum or not and current use of ICS. Salbutamol MDI will be provided as a rescue medication.
Losmapimod (GW856553X)EXPERIMENTALThe subjects will be administered with 7.5 mg (1 tablet) of losmapimod following the completion of the Baseline (time zero) assessments. Subjects will continue to take one tablet in the morning and one tablet in the evening for approximately 2 weeks. After all the pre-dose assessments are completed at the Week 2 visit, subjects will be administered the first 15 mg (2 tablets) dose. Subjects will continue to take two tablets in the morning and two tablets in the evening every day for approximately 22 weeks. Doses of study treatment will be separated by at least 6 hours
losmapimod 2.5 mgEXPERIMENTALlosmapimod 2.5 mg
losmapimod 7.5 mgEXPERIMENTALlosmapimod 7.5 mg
LOSMAPIMOD 7.5 MG TWICE DAILYEXPERIMENTALParticipants received 1 tablet of 7.5 mg Losmapimod orally twice daily, each morning and evening for a period of 12 weeks
LOSMAPIMOD 7.5 MG ONCE DAILYEXPERIMENTALParticipants received 1 tablet of 7.5 mg Losmapimod each morning once daily and placebo tablet each evening once daily orally for a period of 12 weeks.
Losmapimod 20 mgEXPERIMENTALEach subject will receive losmapimod 20 mg QD orally for 5 days, in one of the 4 study periods (per randomization sequence) separated by a minimum washout period of 5 days
Moxifloxacin 400 mgACTIVE_COMPARATOREach subject will receive moxifloxacin 400 mg orally on Day 5, in one of the 4 study periods (per randomization sequence) separated by a minimum washout period of 5 days
2.5 mgEXPERIMENTALLosmapimod for single dose
7.5 mgEXPERIMENTALLosmapimod for single dose
20 mgEXPERIMENTALLosmapimod for single dose
7.5 mg BIDEXPERIMENTALLosmapimod for repeat dose (14 days)
Placebo BIDPLACEBO_COMPARATORPlacebo
1 mg IVEXPERIMENTALUnit Dose Strength: 0.4 mg/mL
?mg IVEXPERIMENTALdose to be determined based on PK of first IV dose
15 mg (oral)EXPERIMENTALtwo 7.5 mg tablets

Interventions

NameTypeDescription
Losmapimod tabletsDRUGLosmapimod tablets will be provided as 15 mg strength in a formulation containing lactose. Administered orally, twice daily approximately 12 hours apart and with food and water for the duration of the treatment period. Participants will be instructed to take their medication with a full glass of water twice-daily within 30 minutes after meals for the duration of their treatment period.
Placebo tabletsDRUGPlacebo tablets will be provided in a formulation containing lactose and visually matching the losmapimod tablets. Administered orally, twice daily approximately 12 hours apart and with food and water for the duration of the treatment period. Participants will be instructed to take their medication with a full glass of water twice-daily within 30 minutes after meals for the duration of their treatment period
Salbutamol MDIDRUGSalbutamol MDI will be provided as a rescue medication.
LosmapimodDRUGLosmapimod (micronized GW856553X) will be supplied as a film coated white, 7 mm round, biconvex, plain faced, tablet. Oral doses of losmapimod, 7.5 mg (1 tablet) or 15 mg (2 tablets), will be taken twice daily (BID) with food and swallowed whole (not chewed or crushed)
placeboDRUGplacebo comparison with active
LOSMAPIMOD 7.5 MGDRUGGW856553 tablets (wet granulation formulation) are available as white, film coated, round, convex tablets manufactured using micronised GW856553X active substance. Tablets are available containing 7.5 mg of GW856553X and are packed into high-density polyethylene (HDPE) bottles.
MoxifloxacinDRUG17.2mm x 7.1 mm capsule shaped pink biconvex tablet of 400 mg unit dose strength. Taken orally 400 mg on Day 5 in one of the 4 study periods
Losmapimod matched PlaceboDRUGDirect compression formulation (visually matched to GW856553), Film coated white, 7 mm round, biconvex, plain faced Tablet. Taken orally for 5 days in one of the 4 study periods
Moxifloxacin PlaceboDRUG16 mm x 8 mm capsule shaped to white film coated tablet. Taken orally for 5 days in one of the 4 study periods
Losmapimod for single doseDRUGFilm coated white tablet
Losmapimod for repeat doseDRUGFilm coated white tablet
losmapimod 1 mgDRUGIV infusion
losmapimod 15 mgDRUGoral, two 7.5 mg tablets
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Eligibility Criteria

Age Range40 Years to N/A
SexALL
Healthy VolunteersNo
Study Sites36

Inclusion Criteria: * COPD diagnosis and severity: Participants with a clinical history of COPD (established by a physician) in accordance with the following definition by the American Thoracic Society/European Respiratory Society, for at least 6 months prior to enrolment. Participants must have ev...

Countries:ArgentinaBrazilBulgariaChileGermanySlovakiaSouth KoreaSpainUnited StatesCanadaCzechiaEstoniaNorwayUkraineUnited KingdomAustralia
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Frequently asked questions about LOSMAPIMOD

What is LOSMAPIMOD used for?

LOSMAPIMOD is an investigational small molecule being developed for cardiovascular and related conditions, including atherosclerosis, focal segmental glomerulosclerosis, chronic obstructive pulmonary disease, acute coronary syndrome, and cardiovascular disease. It is not approved and remains in clinical development.

What does LOSMAPIMOD target?

LOSMAPIMOD is a small molecule that targets p38 MAP kinase, a signaling protein involved in inflammatory responses. By inhibiting this pathway, it is being studied for potential effects in cardiovascular and inflammatory diseases, though its exact mechanism in these conditions is still under investigation.

Who makes LOSMAPIMOD?

LOSMAPIMOD is being developed by GSK plc, a global biopharmaceutical company listed on the London Stock Exchange under the ticker GSK. GSK is conducting clinical trials to evaluate the drug's safety and efficacy in various patient populations.

What phase is LOSMAPIMOD in?

LOSMAPIMOD is in Phase 2 clinical development. It has completed two trials, including a Phase 2 study in atherosclerosis, and several Phase 1 studies. It remains investigational and has not received regulatory approval for any indication.

What clinical trials is LOSMAPIMOD in?

LOSMAPIMOD has been studied in clinical trials including NCT00633022, a Phase 2 FDG-PET/CT imaging study in atherosclerosis, and NCT01039961, a pharmacokinetic study of an IV formulation in cardiovascular disease. Additional Phase 1 trials include NCT01648192 and NCT01756495.

Is LOSMAPIMOD the same as GW856553?

Yes, LOSMAPIMOD is also known as GW856553. Clinical trial records reference both names, with GW856553 appearing in earlier study titles and LOSMAPIMOD used in later trials. Both names refer to the same investigational drug being developed by GSK.