acrivastine
Trade name: Semprex-D
Approved
Mar 25, 1994
Acrivastine is a triprolidine analog antihistamine indicated for the treatment of allergies and hay fever. As an H1 receptor antagonist, it functions by blocking the action of histamine at this receptor thereby preventing the symptoms associated with histamine release such as pruritis, vasodilation, hypotension, edema, bronchoconstriction, and tachycardia. Acrivastine is currently available in combination with pseudoephedrine as the FDA-approved product Semprex-D. It’s used for the relief of symptoms associated with seasonal allergic rhinitis such as sneezing, rhinorrhea, pruritus, lacrimation, and nasal congestion. Acrivastine, a structural analog of triprolidine hydrochloride, exhibits H1-antihistaminic activity in isolated tissues, animals, and humans, and has sedative effects in humans. The propionic acid derivative of acrivastine is a metabolite in several animal species (as well as in man) and also exhibits H1-antihistaminic activity. — NCATS
Clinical trial activity
1 trials · 3 clinical orgs · 3 marketing orgs
Earliest trial started Dec 9, 2020 (NCT04563208)
Timeline
1990s
- Mar 25, 1994
Earliest FDA Approval
- Mar 25, 1994
Auxillium — NDA Secondary Org
- Mar 25, 1994
Endo Pharmaceuticals — NDA Secondary Org
2020s
- Jan 1, 2020
Earliest Phase 2 Sponsor(trial)
Indications
Approved for
Mechanism of action
- Histamine H1 receptorANTAGONIST
HRH1 antagonist
Combination products
semprex
with pseudoephedrine
Approval history
- approvedMar 25, 1994
Chemistry & pharmacology
SMILES
CC1=CC=C(C=C1)C(=C/CN2CCCC2)\C3=CC=CC(\C=C\C(O)=O)=N3- Mol. weight
- 348.4382 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Discontinued
Oral
Yes
Parenteral
No
Topical
No
Sources
- WikipediaAcrivastine ↗
- NCATSA20F9XAI7W ↗
- ChEMBLCHEMBL1224 ↗
Also known as
- (2e)-3-{6-[(1e)-1-(4-methylphenyl)-3-(pyrrolidin-1-yl)prop-1-en-1-yl]pyridin-2-yl}acrylic acid
- (2e)-3-{6-[(1e)-1-(4-methylphenyl)-3-(pyrrolidin-1-yl)prop-1-en-1-yl]pyridin-2-yl}acrylic acid
- 2-propenoic acid, 3-(6-(1-(4-methylphenyl)-3-(1-pyrrolidinyl)-1-propenyl)-2-pyridinyl)-, (e,e)-
- acrivastine
- acrivastine
- acrivastine
- acrivastine
- acrivastine
- acrivastine
- acrivastine
- acrivastine
- benadryl allgy relief plus decongest
- bw-270c
- bw-270c
- bw-270c
- bw-270c
- bw-270c
- bw825c
- bw 825c
- bw-825c
- bw-825c
- bw-825c
- bw-825c
- glaxosmithkline brand of acrivastine
- glaxo wellcome brand of acrivastine
- semprex
- semprex
- semprex
- semprex
- semprex-d
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT04563208 | Phase 2 | Dec 9, 2020 | Ezintsha, SynaVir, University of the Witwatersrand |
Organizations
Research & Development (3)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Ezintsha | Academic/Hospital | 1 | 0 | 1 | 2020 |
| SynaVir | For profit | 1 | 0 | 1 | 2020 |
| University of the Witwatersrand | Academic/Hospital | 1 | 1 | 1 | 2020 |
Marketing (3)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Auxillium | For profit | NDA2 | Mar 25, 1994 |
| Burroughs Wellcome | For profit | NDA | — |
| Endo Pharmaceuticals | For profit | NDA2 | Mar 25, 1994 |