Approval Probability
TA Base Rate
Adjusted LOA
ML Risk
Also known as Tredaptive, MK0524A
niacin laropiprant · 13 trials · 10 indications
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.
Blood samples taken at baseline and after 12 weeks of treatment to determine the LDL-C and HDL-C levels. The LDL-C/HDL-C ratio was then calculated for baseline and Week 12 and the change from baseline at Week 12 was recorded.
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.
The creatinine-normalized urine levels of 11-dTxB2 on Day 7 following a 7 day course of daily dosing in the overall 24 hour collection interval
Measure of rate of absorption of ER niacin
Measure of extent of absorption of ER niacin
Measure of extent of absorption of laropiprant
Measure of rate of absorption of laropiprant
| Arm | Type | Description |
|---|---|---|
| ERN/LRPT | EXPERIMENTAL | One 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 ERN | EXPERIMENTAL | One 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. |
| Placebo | PLACEBO_COMPARATOR | One tablet placebo to ERN/LRPT once daily for 4 weeks, then two tablets placebo to ERN/LRPT daily for 28 weeks. |
| Placebo → MK-0524A 2g | PLACEBO_COMPARATOR | Following an 8-week active run-in (MK-0524A 1g (4 Weeks) then MK-0524A 2g (4 weeks) participants will be administered MK-0524A Placebo for 5 days (drug holiday) followed by MK-0524A 2 g for the remainder of the study (7 days). |
| Placebo → Extended Release (ER)-Niacin 2g | ACTIVE_COMPARATOR | Following an 8-week active run-in (MK-0524A 1g (4 Weeks) then MK-0524A 2g (4 weeks) participants will be administered MK-0524A Placebo for 5 days (drug holiday) followed by ER-Niacin 2g for the remainder of the study (7 days) |
| MK-0524A 2g | EXPERIMENTAL | Following an 8-week active run-in (MK-0524A 1g (4 Weeks) then MK-0524A 2g (4 weeks) participants will be administered MK-0524A 2g for the remainder of the study (approximately 2 weeks). |
| MK-0524B 2g/20 mg | EXPERIMENTAL | Co-administration of one tablet of MK-0524A (Extended Release \[ER\] niacin/laropiprant \[LRPT\] 1g + one tablet of simvastatin 10 mg for 4 weeks, then co-administration of two tablets of MK-0524A 1g + simvastatin 20 mg for 8 weeks |
| MK-0524B 2g/40mg | EXPERIMENTAL | Co-administration of one tablet of MK-0524A 1g + one tablet of simvastatin 20 mg for 4 weeks, then co-administration of two tablets of MK-0524A 1g + simvastatin 40 mg for 8 weeks |
| Atorvastatin 10 mg | ACTIVE_COMPARATOR | Atorvastatin 10 mg, orally, once daily for 12 weeks |
| Atorvastatin 20 mg | ACTIVE_COMPARATOR | Atorvastatin 20 mg, orally, once daily for 12 weeks |
| Atorvastatin 40 mg | ACTIVE_COMPARATOR | Atorvastatin 40 mg, orally, once daily for 12 weeks |
| Atorvastatin 80 mg | ACTIVE_COMPARATOR | Atorvastatin 80 mg, orally, once daily for 12 weeks |
| Period 1 | EXPERIMENTAL | In 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 2 | EXPERIMENTAL | In 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 3 | EXPERIMENTAL | - |
| A | EXPERIMENTAL | Arm A: ER niacin/laropiprant + Placebo to laropiprant |
| B | EXPERIMENTAL | Arm B: ER niacin + Placebo to laropiprant |
| C | EXPERIMENTAL | Arm C: laropiprant + Placebo to ER Niacin/laropiprant |
| D | PLACEBO_COMPARATOR | Arm D: Placebo |
| Name | Type | Description |
|---|---|---|
| ER niacin (+) laropiprant (ERN/LRPT) | DRUG | One 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) | DRUG | Two 1g tablets ERN (2g total) once daily for 12 weeks. |
| Placebo to ERN/LRPT | DRUG | One tablet placebo to ERN/LRPT once daily for 4 weeks, then two tablets placebo to ERN/LRPT daily for 28 weeks |
| MK0524A, /Duration of Treatment : 4 Weeks | DRUG | - |
| Comparator : niacin /Duration of Treatment : 1 Weeks | DRUG | - |
| niacin (+) laropiprant | DRUG | Duration of Treatment: 18 Weeks |
| niacin | DRUG | Duration of Treatment: 18 Weeks |
| MK-0524A | DRUG | - |
| ER Niacin | DRUG | - |
| Placebo | DRUG | - |
| Atorvastatin | DRUG | - |
| Simvastatin | DRUG | - |
| ER-niacin | DRUG | Duration of Treatment - 24 weeks |
| Comparator: placebo (unspecified) | DRUG | - |
| Comparator : placebo (unspecified) / Duraton of Treatment: 4 Weeks | DRUG | - |
| MK0524A, niacin (+) laropiprant / Duration of Treatment : 4 Weeks | DRUG | - |
| Comparator : niacin / Duraton of Treatment: 4 Weeks | DRUG | - |
| MK0524A, /Duration of Treatment : 8 Weeks | DRUG | - |
| Comparator : placebo (unspecified) /Duration of Treatment : 8 Weeks | DRUG | - |
| Comparator: niacin / Duration of Treatment: 17 Weeks | DRUG | - |
| MK0524A, niacin (+) laropiprant / Duration of Treatment: 17 Weeks | DRUG | - |
| Comparator: placebo (unspecified) / Duration of Treatment: 17 Weeks | DRUG | - |
| Comparator: aspirin | DRUG | 81 mg oral tablet once daily for 7 days |
| Comparator: clopidogrel | DRUG | 75 mg oral tablet once daily for 7 days |
| Comparator: laropiprant | DRUG | 40 mg oral tablet once daily for 7 days |
| Comparator: placebo | DRUG | placebo oral tablet once daily for 7 days |
| Comparator: ER niacin (+) laropiprant | DRUG | ER niacin 2 g/ laropiprant 40 mg daily for 7 days. |
| Comparator: ER niacin | DRUG | ER niacin 2 g daily for 7 days. |
| niacin (+) laropiprant (Source 1) | DRUG | Single dose of MK0524A (ER Niacin/laropiprant 1000/20 mg) from Source 1 in one of two treatment periods. |
| Comparator: niacin (+) laropiprant (Source 2) | DRUG | Single dose of MK0524A (ER Niacin/laropiprant 1000/20 mg) from Source 2 in one of two treatment periods. |
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...
Top 7 of 10 competitors
| Company | Ticker | Trials | Lead Phase | Drugs |
|---|---|---|---|---|
| Merck & Co., Inc. | MRK | 2 | PHASE3 | Enlicitide |
| Eli Lilly and Company | LLY | 2 | PHASE3 | Lepodisiran, Muvalaplin |
| Novartis AG Sponsored ADR | NVS | 2 | PHASE3 | Pelacarsen |
| NewAmsterdam Pharma Company N.V. | NAMS | 3 | PHASE3 | Obicetrapib |
| AstraZeneca PLC | AZN | 2 | PHASE2 | Rosuvastatin, AZD0780, AZD4954 |
| Arrowhead Pharmaceuticals, Inc. | ARWR | 1 | PHASE1 | ARO-DIMERPA |
| CRISPR Therapeutics AG | CRSP | 1 | PHASE1 | CTX310 |
Niacin laropiprant is an investigational small molecule combination developed by Merck & Company, Inc. (MRK) for dyslipidemia and hypercholesterolemia. It pairs extended-release niacin with laropiprant and was studied in Phase 3 clinical development. It is not described as approved and remains an investigational therapy.
Niacin laropiprant was developed for dyslipidemia, hypercholesterolemia, primary hypercholesterolemia, and type 2 diabetes mellitus. These are the conditions studied across its clinical program. It is an investigational combination therapy, not a marketed product, and its development focused on lipid management in these patient populations.
Merck & Company, Inc., which trades under the ticker MRK, developed niacin laropiprant. The company sponsored the clinical program for the combination, including the Phase 3 dyslipidemia study and the supporting Phase 1 trials. Merck is the developer associated with this asset.
Niacin laropiprant reached Phase 3 clinical development. Its Phase 3 study in dyslipidemia was completed, and the program also included completed Phase 1 trials. The drug is investigational and is not described as FDA approved.
Niacin laropiprant was studied in completed trials including NCT00961636, a Phase 3 long-term study in dyslipidemia with 1,152 patients, and NCT01012219, a Phase 1 study of laropiprant with clopidogrel and aspirin. Other completed trials include NCT00944645 and NCT00618995. All trials in the program are completed.