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niacin laropiprant

Phase 3

Dyslipidemia | Small molecule | Cardiovascular |Merck & Company, Inc.|Last Updated: Feb 17, 2017

Success Probability

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Market & Valuation

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Trial Design

RandomizedDouble-BlindACTIVE_CONTROLLED
Total Trials3
Total Enrollment1,915

FDA Designations

No designations recorded

Clinical trial landscape

niacin laropiprant · 7 trials · 8 indications

Phase 3 4Phase 2 1Phase 1 2
NCT00961636A Long-term Study of ERN/LRPT (Extended Release Niacin/Laropiprant [MK0524A]) in Patients With Dyslipidemia (0524A-102)Dyslipidemia
COMPLETED1,152 Analytics
NCT00479388Study of Extended Release Niacin/Laropiprant on Lipids (0524A-067)Primary Hypercholesterolemia
COMPLETED1,216 Analytics
NCT00378833Tolerability of MK0524A Versus Niacin Extended-Release (0524A-054)Hypercholesterolemia
COMPLETED1,300 Analytics
NCT00269204Lipid Efficacy/Tolerability Study (0524A-020)Primary Hypercholesterolaemia
COMPLETED1,620 Analytics
PHASE3COMPLETED
A Long-term Study of ERN/LRPT (Extended Release Niacin/Laropiprant [MK0524A]) in Patients With Dyslipidemia (0524A-102)
DyslipidemiaUnlock trial analytics
PHASE3COMPLETED
Study of Extended Release Niacin/Laropiprant on Lipids (0524A-067)
Primary HypercholesterolemiaUnlock trial analytics
PHASE3COMPLETED
Tolerability of MK0524A Versus Niacin Extended-Release (0524A-054)
HypercholesterolemiaUnlock trial analytics
PHASE3COMPLETED
Lipid Efficacy/Tolerability Study (0524A-020)
Primary HypercholesterolaemiaUnlock trial analytics

Study Endpoints

Primary Endpoints

Number Participants With Days Per Week With Global Flushing Severity Score (GFSS) ≥4 Partitioned Into 6 Categories During the Postwithdrawal Period
Week 21 to Week 32

Flushing symptoms were recorded using participant's response to the Global Flushing Severity Score (GFSS), which assessed the overall severity of the flushing experience, using a scale of 0 (no symptom) to 10 (extreme). The number of days/week was derived as: 7\*(total number of days with GFSS ≥4 across Weeks 21-32 divided by the total number of days with nonmissing GFSS across the same period). The number of days/week with a GFSS ≥4 for each participant was listed in 1 of the following 6 categories: 0, \>0 to 0.5, \>0.5 to 1, \>1 to 2, \>2 to 3, and \>3 days per week.

Percent Change From Baseline in Low Density Lipoprotein Cholesterol at Week 12
Baseline and 12 Weeks
Global Flushing Severity Score (GFSS) over 16 weeks
Reductions of LDL-C concentrations at 24 weeks and better tolerability
at 24 weeks
Acute cutaneous symptoms induced by niacin for 7 days.
7 days
Cutaneous Bleeding Time (BT)
Day 8

Cutaneous bleeding Time (BT) on Day 8 after daily administration of laropiprant with aspirin and clopidogrel for 7 days versus BT on Day 8 after daily administration of placebo with aspirin and clopidogrel for 7 days. The model used included treatment, period and sequence as fixed effect variables and subjects as the random effect variable. Period 3 was not analyzed as bleeding time was not an objective for this part of the study.

Maximum Plasma Concentration (Cmax) of Nicotinuric Acid
Predose and up to 24 hours postdose

Measure of rate of absorption of ER niacin

Total Amount of Urinary Excretion of Niacin and Its Metabolites
Predose and up to 96 hours postdose

Measure of extent of absorption of ER niacin

Area Under Curve (AUC 0-infinity) of Laropiprant
Predose and up to 48 hours postdose

Measure of extent of absorption of laropiprant

Maximum Concentration (Cmax) of Laropiprant
Predose and up to 48 hours postdose

Measure of rate of absorption of laropiprant

Secondary Endpoints

Number of Participants With Maximum GFSS ≥4 During the Post-withdrawal Period
Week 21 to Week 32
Percent Change From Baseline in High Density Lipoprotein Cholesterol at Week 12
Baseline and 12 Weeks
Percent Change From Baseline in Triglycerides at Week 12
Baseline and 12 Weeks
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Study Design & Arms

AllocationRANDOMIZED
MaskingDOUBLE
ModelPARALLEL
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
ERN/LRPTEXPERIMENTALOne 1g/20 mg tablet ERN/LRPT once daily for 4 weeks, then two 1g/20 mg tablets daily (2g/40 mg total) for 28 weeks
ERN/LRPT then ERNEXPERIMENTALOne 1g/20mg tablet ERN/LRPT once daily for 4 weeks, then two 1g/20 mg tablets daily (2g/40 mg total) for 16 weeks then Two 1g tablets ERN (2g total) once daily for 12 weeks.
PlaceboPLACEBO_COMPARATOROne tablet placebo to ERN/LRPT once daily for 4 weeks, then two tablets placebo to ERN/LRPT daily for 28 weeks.
1OTHEROne tablet of ER niacin/ laropiprant (1g) + one tablet of the run-in statin dose, titrating up to ER niacin/laropiprant (2g) at Week 4 for an additional 8 weeks, with no adjustments to the run-in statin dose.
2ACTIVE_COMPARATORStable dose of simvastatin or atorvastatin (20mg to 40mg) for 12 weeks.
Period 1EXPERIMENTALIn Periods 1 and 2 each participant will receive one of the following treatments in a randomized crossover fashion: Treatment A (aspirin 81 mg, clopidogrel 75 mg and laropiprant 40 mg once daily for 7 days) or Treatment B (aspirin 81 mg, clopidogrel 75 mg and placebo to laropiprant 40 mg once daily for 7 days).
Period 2EXPERIMENTALIn Periods 1 and 2 each participant will receive one of the following treatments in a randomized crossover fashion: Treatment A (aspirin 81 mg, clopidogrel 75 mg and laropiprant 40 mg once daily for 7 days) or Treatment B (aspirin 81 mg, clopidogrel 75 mg and placebo to laropiprant 40 mg once daily for 7 days).
Period 3EXPERIMENTAL -
AACTIVE_COMPARATORMK0524A Source 1 (Phase III manufacturing site)
BACTIVE_COMPARATORMK0524A Source 2 (commercial manufacturing site)

Interventions

NameTypeDescription
ER niacin (+) laropiprant (ERN/LRPT)DRUGOne 1g/20 mg tablet ERN/LRPT once daily for 4 weeks, then two 1g/20 mg tablets daily (2g/40 mg total) for 28 weeks
Extended-release niacin (ERN)DRUGTwo 1g tablets ERN (2g total) once daily for 12 weeks.
Placebo to ERN/LRPTDRUGOne tablet placebo to ERN/LRPT once daily for 4 weeks, then two tablets placebo to ERN/LRPT daily for 28 weeks
Comparator: simvastatinDRUGsimvastatin (20mg to 40mg) for 12 weeks.
niacin (+) laropiprantDRUGOne tablet of ER niacin/ laropiprant (1g); titrating up to ER niacin/laropiprant (2g) at Week 4 for an additional 8 weeks, with no adjustments to the run-in statin dose.
Comparator: atorvastatin calciumDRUGatorvastatin calcium (20mg to 40mg) for 12 weeks.
niacinDRUGDuration of Treatment: 18 Weeks
ER-niacinDRUGDuration of Treatment - 24 weeks
Comparator: placebo (unspecified)DRUG -
Comparator: aspirinDRUG81 mg oral tablet once daily for 7 days
Comparator: clopidogrelDRUG75 mg oral tablet once daily for 7 days
Comparator: laropiprantDRUG40 mg oral tablet once daily for 7 days
Comparator: placeboDRUGplacebo oral tablet once daily for 7 days
niacin (+) laropiprant (Source 1)DRUGSingle dose of MK0524A (ER Niacin/laropiprant 1000/20 mg) from Source 1 in one of two treatment periods.
Comparator: niacin (+) laropiprant (Source 2)DRUGSingle dose of MK0524A (ER Niacin/laropiprant 1000/20 mg) from Source 2 in one of two treatment periods.
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Eligibility Criteria

Age Range18 Years to 75 Years
SexALL
Healthy VolunteersNo

Inclusion Criteria: * Patient is a male, or a female who is unlikely to conceive, as indicated by meeting at least one of the following conditions: (a) Patient is a male.(b) Patient is a female of reproductive potential and either agrees to remain abstinent (if this form of birth control is accepte...

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Frequently asked questions about niacin laropiprant

What is niacin laropiprant used for?

Niacin laropiprant is an investigational small molecule being studied for dyslipidemia, hypercholesterolemia, type 2 diabetes mellitus, and primary hypercholesterolemia. It is being developed by Merck & Company, Inc. (MRK) as a potential treatment for these metabolic conditions.

How does niacin laropiprant work?

Niacin laropiprant combines niacin, which affects lipid metabolism, with laropiprant, a prostaglandin D2 receptor antagonist. The laropiprant component is intended to reduce the flushing side effect associated with niacin therapy. This combination is being studied for its effects on lipid levels in patients with dyslipidemia and related conditions.

Who makes niacin laropiprant?

Niacin laropiprant is being developed by Merck & Company, Inc., a pharmaceutical company traded on the New York Stock Exchange under the ticker symbol MRK. The drug is an investigational combination product being evaluated for metabolic indications.

What phase is niacin laropiprant in?

Niacin laropiprant is in Phase 1 clinical development. It has completed three clinical trials, including Phase 1, Phase 2, and Phase 3 studies, but is not approved by the FDA and remains investigational. All completed trials have finished, with no active trials currently ongoing.

What clinical trials is niacin laropiprant in?

Niacin laropiprant has completed three clinical trials: NCT00111891, a Phase 2 study in dyslipidemia with 575 participants; NCT00269204, a Phase 3 study in primary hypercholesterolaemia and mixed hyperlipidaemia with 1620 participants; and NCT00944645, a Phase 1 bioequivalence study in dyslipidemia with 188 participants. All trials are completed.

Is niacin laropiprant the same as MK0524A?

Yes, niacin laropiprant is also known as MK0524A, which is the combination of extended release niacin and laropiprant. Clinical trials reference MK0524A in their titles, including NCT00944645 and NCT00961636, which study this combination product for dyslipidemia.