eletriptan
Trade name: relpax
Approved
Dec 26, 2002
Eletriptan (eletriptan hydrobromide, trade name Relpax) is a selective 5-hydroxytryptamine (5-HT1B/1D) serotonin receptor agonist (triptan) indicated for the acute treatment of migraine with or without aura in adults. Eletriptan binds with high affinity to 5-HT1B, 5-HT1D and 5-HT1F receptors, and has modest affinity for 5-HT1A, 5-HT1E, 5-HT2B and 5-HT7 receptors. The therapeutic activity of eletriptan for the treatment of migraine headache is thought to be due to the agonist effects at the 5-HT1B/1D receptors on intracranial blood vessels (including the arterio-venous anastomoses) and sensory nerves of the trigeminal system which result in cranial vessel constriction and inhibition of pro-inflammatory neuropeptide release. Eletriptan (Relpax) has been approved for use in the acute treatment of migraine in 51 countries and has been introduced in 17 countries including Mexico, Italy, France and Japan. — NCATS
Clinical trial activity
15 trials · 7 clinical orgs · 15 marketing orgs
Earliest trial started Jul 1, 1996 (NCT01978496)
Timeline
2000s
2010s
- Jul 29, 2013
Apotex — Marketing Organization
- Jun 16, 2017
Zydus Discovery DMCC — Marketing Organization
- Jun 27, 2017
Teva — Marketing Organization
- Aug 11, 2017
Mylan — Marketing Organization
- Aug 29, 2017
Ajanta Pharma Ltd — Marketing Organization
- Aug 29, 2017
Chartwell Pharmaceuticals — Marketing Organization
- May 25, 2018
Amneal Pharmaceuticals — Marketing Organization
- May 25, 2018
Jerome Stevens Pharmaceuticals — Marketing Organization
- Jan 15, 2019
Aurobindo Pharma — Marketing Organization
2020s
- Jul 13, 2020
Yung Shin Pharm. Ind. Co., Ltd. — Marketing Organization
- Jul 13, 2022
Beximco — Marketing Organization
- Jul 7, 2025
Annora Pharma — Marketing Organization
Indications
Mechanism of action
HTR1B agonist
Selective
HTR1F agonist
Selective
HTR1D agonist
Selective
Approval history
- approvedDec 26, 2002
Chemistry & pharmacology
SMILES
CN1CCC[C@@H]1Cc1c[nH]c2ccc(CCS(=O)(=O)c3ccccc3)cc12- Mol. weight
- 382.53 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL1510 ↗
- WikipediaEletriptan ↗
- NCATS22QOO9B8KI ↗
- ChEMBLCHEMBL1201003 ↗
Also known as
- 3-(1-methyl-2-pyrrolidinylmethyl)-5-(2-(phenylsulfonyl)ethyl)-1h-indole hydrobromide
- eletriptan
- eletriptan
- eletriptan
- eletriptan
- eletriptan
- eletriptan
- eletriptan
- eletriptan
- eletriptan
- eletriptan
- eletriptan hydrobromide
- eletriptan hydrobromide
- eletriptan hydrobromide
- eletriptan hydrobromide
- eletriptan hydrobromide
- eletriptanum
- eletriptanum
- (r)-3-((1-methyl-2-pyrrolidinyl)methyl)-5-(2-(phenylsulfonyl)ethyl)-1h-indole
- (r)-3-((1-methyl-2-pyrrolidinyl)methyl)-5-(2-(phenylsulfonyl)ethyl)-1h-indole monohydrobromide
- relpax
- relpax
- relpax
- relpax
- relpax
- uk-116044
- uk-116044
- uk-116,044
- uk 116044-04
- uk-11604404
- uk-11604404
- uk-116,044-04
- uk-116044-04
- uk-116044-04
- uk-116044-04
- uk-116044-04 [as hydrobromide)
- uk-116044-04 [as hydrobromide)
- uk 166044
- uk 166,044
- uk-166044
- uk-166,044
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT01619176 | N/A | Oct 1, 2012 | Chinese Academy of Medical Sciences, Jiao Tong University |
| NCT01139515 | Phase 1 | Jul 1, 2010 | Pfizer |
| NCT00871806 | Phase 1 | Apr 1, 2009 | Pfizer |
| NCT00751803 | Phase 2 | Aug 1, 2008 | Boehringer Ingelheim |
| NCT01276977 | N/A | Apr 1, 2008 | California Medical Clinic for Headache |
| NCT00385008 | Phase 3 | Sep 1, 2006 | GlaxoSmithKline |
| NCT00174395 | Phase 4 | Mar 1, 2005 | Pfizer |
| NCT00259649 | Phase 4 | Aug 1, 2004 | Pfizer, University of Pittsburgh |
| NCT00632385 | Phase 4 | Jan 1, 2003 | Pfizer |
| NCT00634985 | Phase 4 | Nov 1, 2002 | Pfizer |
| NCT01859481 | Phase 3 | Mar 1, 2000 | Pfizer |
| NCT01989936 | Phase 3 | Jan 1, 1999 | Pfizer |
| NCT01986270 | Phase 3 | Dec 1, 1996 | Pfizer |
| NCT01986088 | Phase 3 | Nov 1, 1996 | Pfizer |
| NCT01978496 | Phase 3 | Jul 1, 1996 | Pfizer |
Organizations
Research & Development (7)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Pfizer | For profit | 11 | 10 | 3 | 1996 |
| Boehringer Ingelheim | For profit | 1 | 1 | 1 | 2008 |
| California Medical Clinic for Headache | Academic/Hospital | 1 | 1 | 1 | 2008 |
| Chinese Academy of Medical Sciences | Academic/Hospital | 1 | 1 | 1 | 2012 |
| GlaxoSmithKline | For profit | 1 | 1 | 1 | 2006 |
| Jiao Tong University | Academic/Hospital | 1 | 0 | 1 | 2012 |
| University of Pittsburgh | Academic/Hospital | 1 | 1 | 1 | 2004 |
Marketing (18)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Ajanta Pharma Ltd | For profit | MKTG | Aug 29, 2017 |
| Amneal Pharmaceuticals | For profit | MKTG | May 25, 2018 |
| Annora Pharma | For profit | MKTG | Jul 7, 2025 |
| Apotex | For profit | MKTG | Jul 29, 2013 |
| Aurobindo Pharma | For profit | SYN | Jan 15, 2019 |
| Aurobindo Pharma | For profit | MKTG | Jan 15, 2019 |
| Beximco | For profit | MKTG | Jul 13, 2022 |
| Chartwell Pharmaceuticals | For profit | MKTG | Aug 29, 2017 |
| Jerome Stevens Pharmaceuticals | For profit | MKTG | May 25, 2018 |
| Mylan | For profit | MKTG | Aug 11, 2017 |
| Mylan | For profit | SYN | Aug 11, 2017 |
| Pfizer | For profit | SYN | Dec 26, 2002 |
| Pfizer | For profit | NDA | Dec 26, 2002 |
| Pharmacia | For profit | NDA2 | Dec 26, 2002 |
| Teva | For profit | MKTG | Jun 27, 2017 |
| Upjohn | For profit | MKTG | Dec 26, 2002 |
| Yung Shin Pharm. Ind. Co., Ltd. | For profit | MKTG | Jul 13, 2020 |
| Zydus Discovery DMCC | For profit | MKTG | Jun 16, 2017 |