pemirolast
Trade name: alamast
Approved
Sep 24, 1999
Pemirolast is a mast cell stabilizer that acts as an antiallergic agent, it is approved in Japan for the treatment of bronchial asthma and of allergic rhinitis. Pemirolast strongly inhibits extracellular Ca2+ influx and the release of intracellular Ca2+, an important factor in the release of chemical mediators, by inhibiting inositol-phospholipid metabolism in mast cells. It also inhibits the release of arachidonic acid. Furthermore contribution of increasing effect on c-AMP based on inhibiting phosphodiesterase is suggested. Main pharmacological effects is an inhibition of release of chemical mediators, e.g. histamine, LTB4, LTC4, LTD4, PGD2, TXB2 and PAF from human lung tissues, abraded fragments of the nasal mucosa, and peripheral leukocytes, rat peritoneal exudate cells, and rat and guniea pig lung tissues. — NCATS
Clinical trial activity
7 trials · 5 clinical orgs · 1 marketing orgs
Earliest trial started May 13, 2011 (NCT01354184)
Timeline
1990s
- Sep 24, 1999
Santen Inc. — Earliest FDA Approval
- Sep 24, 1999
Santen Inc. — NDA Secondary Org
- Sep 24, 1999
Santen Inc. — NDA Organization
Indications
Approved for
Mechanism of action
- Unspecified targetOTHER
Unknown
Mode of action not fully understood; it seems to inhibit calcium influx into mast cells, stabilizing them
Approval history
- approvedPriority reviewSep 24, 1999
Chemistry & pharmacology
SMILES
Cc1cccn2c(=O)c(-c3nnn[nH]3)cnc12- Mol. weight
- 228.22 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
- Delivery
- Topical
- Availability
- Discontinued
Oral
No
Parenteral
No
Topical
Yes
Sources
- ChEMBLCHEMBL1201198 ↗
- WikipediaPemirolast ↗
- NCATS2C09NV773M ↗
- ChEMBLCHEMBL1201050 ↗
Also known as
- 9-methyl-3-(1h-tetrazol-5-yl)-4h-pyrido(1,2-a)pyrimidin-4-one
- 9-tbx
- alamast
- alamast
- alamast
- alamast
- alamast
- alamast
- alamast
- alegysal
- bmy 26517
- bmy-26517
- bmy-26517
- bmy-26517
- pemirolast
- pemirolast
- pemirolast
- pemirolast
- pemirolast
- pemirolast
- pemirolast
- pemirolast
- pemirolast
- pemirolast potassium
- pemirolast potassium
- pemirolast potassium
- pemirolast potassium
- pemirolast potassium salt
- pemirolastum
- pemirolastum
- pemirox
- pemirox
- potassium pemirolast
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT03119714 | Phase 2 | Nov 1, 2016 | Karolinska Institute, University of Amsterdam, University of Gothenburg |
| NCT02615080 | Phase 2 | Nov 30, 2015 | RSPR Pharma AB, University of Copenhagen |
| NCT02609334 | Phase 2 | Mar 1, 2015 | RSPR Pharma AB, University of Copenhagen |
| NCT02517372 | Phase 1 | Oct 1, 2014 | RSPR Pharma AB |
| NCT01723618 | Phase 1 | Nov 1, 2012 | RSPR Pharma AB |
| NCT01540604 | Phase 2 | Feb 23, 2012 | Karolinska Institute, RSPR Pharma AB |
| NCT01354184 | Phase 2 | May 13, 2011 | RSPR Pharma AB, University of Copenhagen |
Organizations
Research & Development (5)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| RSPR Pharma AB | For profit | 6 | 6 | 2 | 2011 |
| University of Copenhagen | Academic/Hospital | 3 | 0 | 1 | 2011 |
| Karolinska Institute | Academic/Hospital | 2 | 1 | 1 | 2012 |
| University of Amsterdam | Academic/Hospital | 1 | 0 | 1 | 2016 |
| University of Gothenburg | Academic/Hospital | 1 | 0 | 1 | 2016 |
Marketing (2)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Santen Inc. | For profit | NDA2 | Sep 24, 1999 |
| Santen Inc. | For profit | NDA | Sep 24, 1999 |