olbetam
Acipimox is a niacin derivative used as a lipid-lowering agent. It reduces triglyceride levels and increases HDL cholesterol. It may have less marked adverse effects than niacin, although it is unclear whether the recommended dose is as effective as standard doses of niacin. — Wikipedia
Clinical trial activity
20 trials · 12 clinical orgs · 0 marketing orgs
Earliest trial started Sep 1, 2002 (NCT00246402)
Timeline
Indications
Studied for
- Bulimia Nervosa · Phase 2
- Diabetes Mellitus, Type 1 · Phase 3
- Diabetes Mellitus, Type 2 · Phase 2/Phase 3
- Feeding and Eating Disorders · Phase 2
- Healthy Volunteers · Phase 1
- Heart Failure · Phase 2
- Hypertriglyceridemia · Phase 2
- Insulin Resistance · Phase 2
- Metabolic Syndrome · Phase 2/Phase 3
- Obesity, Abdominal · Phase 2
Mechanism of action
- Carbonic anhydraseINHIBITOR
Carbonic anhydrase inhibitor
Acipimox is a hypolipidemic agent. It has special application for the treatment of hyperlipidemia in non-insulin-dependent diabetic patients. Acipimox acts on the niacin receptor 1, inhibiting the enzyme triglyceride lipase. This reduces the concentration of fatty acids in the blood plasma and their inflow into the liver. Consequently, VLDL cholesterol production in the liver is reduced, which leads indirectly to a reduction in LDL and increase in HDL cholesterol (Wikipedia).
- Carbonic anhydrase 2 (CA2) ↗
- Carbonic anhydrase 7 (CA7) ↗
- Carbonic anhydrase 1 (CA1) ↗
- Carbonic anhydrase 3 (CA3) ↗
- Carbonic anhydrase 6 (CA6) ↗
- Carbonic anhydrase 12 (CA12) ↗
- Carbonic anhydrase 14 (CA14) ↗
- Carbonic anhydrase 9 (CA9) ↗
- Carbonic anhydrase 4 (CA4) ↗
- Carbonic anhydrase 13 (CA13) ↗
- Carbonic anhydrase 5B, mitochondrial (CA5B) ↗
- Carbonic anhydrase 5A, mitochondrial (CA5A) ↗
- Carbonic anhydrase II
- Carbonic anhydrase III
- Carbonic anhydrase VI
- Carbonic anhydrase I
- Carbonic anhydrase VB
- Carbonic anhydrase VA
- Carbonic anhydrase VII
- Carbonic anhydrase XIV
- Carbonic anhydrase XII
- Carbonic anhydrase IV
- Carbonic anhydrase XIII
- Carbonic anhydrase IX
- Carbonic anhydrases; II & IX
- Carbonic anhydrase V
- Unspecified targetOTHER
Unknown
Acipimox is a hypolipidemic agent. It has special application for the treatment of hyperlipidemia in non-insulin-dependent diabetic patients. Acipimox acts on the niacin receptor 1, inhibiting the enzyme triglyceride lipase. This reduces the concentration of fatty acids in the blood plasma and their inflow into the liver. Consequently, VLDL cholesterol production in the liver is reduced, which leads indirectly to a reduction in LDL and increase in HDL cholesterol (Wikipedia).
- Unspecified targetUnknown
Unknown
Acipimox is a hypolipidemic agent. It has special application for the treatment of hyperlipidemia in non-insulin-dependent diabetic patients. Acipimox acts on the niacin receptor 1, inhibiting the enzyme triglyceride lipase. This reduces the concentration of fatty acids in the blood plasma and their inflow into the liver. Consequently, VLDL cholesterol production in the liver is reduced, which leads indirectly to a reduction in LDL and increase in HDL cholesterol (Wikipedia).
Chemistry & pharmacology
SMILES
Cc1cnc(C(=O)O)c[n+]1[O-]- Mol. weight
- 154.12 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaAcipimox ↗
- ChEMBLCHEMBL345714 ↗
Also known as
- 5-methylpyrazine-2-carboxylic acid 4-oxide
- 5-methylpyrazinecarboxylic acid 4-oxide
- acipimox
- acipimox
- acipimox
- acipimox
- acipimox
- acipimox
- acipimox
- acipimox
- methylpyrazinecarboxylic acid 4-oxide
- nedios
- olbemox
- olbemox
- olbetam
- olbetam
- olbetam
- olbetam
- olbetam
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT03325491 | N/A | Mar 7, 2018 | University of Exeter |
| NCT02980952 | N/A | Jan 1, 2017 | University of Exeter |
| NCT02792621 | N/A | Nov 8, 2016 | University of Exeter |
| NCT02796950 | N/A | Jun 1, 2016 | Aarhus University |
| NCT02782208 | N/A | May 1, 2016 | Aarhus University |
| NCT01980524 | Phase 2/Phase 3 (Phase 3) | Oct 1, 2013 | University of Vienna |
| NCT01209416 | N/A | Jun 1, 2012 | Aarhus University |
| NCT01488409 | Phase 2 | May 1, 2012 | American Diabetes Association, Harvard University |
| NCT01580813 | N/A | Jun 1, 2011 | Department of Veteran Affairs, Pfizer, University of Colorado, Denver |
| NCT01816165 | Phase 3 | Jun 1, 2011 | University of Colorado, Denver |
| NCT01260376 | N/A | Apr 1, 2011 | Aarhus University |
| NCT01299831 | N/A | Jan 1, 2011 | Aarhus University |
| NCT00943059 | N/A | Mar 1, 2010 | Maastricht University |
| NCT00549614 | N/A | Oct 1, 2007 | Aarhus University |
| NCT00449423 | Phase 2 | Mar 1, 2007 | Aarhus University |
| NCT00759291 | Phase 2/Phase 3 (Phase 3) | Apr 1, 2006 | Harvard University |
| NCT02256722 | Phase 1 | Oct 1, 2005 | Boehringer Ingelheim |
| NCT00153179 | Phase 1/Phase 2 (Phase 2) | Sep 1, 2005 | Harvard University |
| NCT03338387 | Phase 2 | May 6, 2003 | Charles University |
| NCT00246402 | N/A | Sep 1, 2002 | Harvard University, National Heart, Lung, and Blood Institute (NHLBI) |
Organizations
Research & Development (12)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Aarhus University | Academic/Hospital | 7 | 7 | 2 | 2007 |
| Harvard University | Academic/Hospital | 4 | 3 | 3 | 2002 |
| University of Exeter | Academic/Hospital | 3 | 3 | 1 | 2016 |
| University of Colorado, Denver | Academic/Hospital | 2 | 2 | 2 | 2011 |
| American Diabetes Association | Academic/Hospital | 1 | 0 | 1 | 2012 |
| Boehringer Ingelheim | For profit | 1 | 1 | 1 | 2005 |
| Charles University | Academic/Hospital | 1 | 1 | 1 | 2003 |
| Department of Veteran Affairs | Government | 1 | 0 | 1 | 2011 |
| Maastricht University | Academic/Hospital | 1 | 1 | 1 | 2010 |
| National Heart, Lung, and Blood Institute (NHLBI) | Government | 1 | 1 | 1 | 2002 |
| Pfizer | For profit | 1 | 0 | 1 | 2011 |
| University of Vienna | Academic/Hospital | 1 | 1 | 1 | 2013 |