astemizole

Trade name: Hismanal

Small moleculewithdrawn

Approved

Jun 1, 1988

Astemizole is antihistamine drug, discovered by Janssen Pharmaceutical and used to prevent sneezing, runny nose, itching and watering of the eyes, and other allergic symptoms. The drug was withdrawn from U.S. market in 1999 due to the potential to cause arrhythmias at high doses. — NCATS

Clinical trial activity

0 trials · 0 clinical orgs · 1 marketing orgs

Phase 1

Phase 2

Phase 3

Phase 4

Timeline

1970s

Jun 1, 1977
Johnson and Johnson — First NDA Organization
Jun 1, 1977
Johnson and Johnson — NDA Organization

1980s

Jun 1, 1988
Earliest FDA Approval

Indications

Approved for

Rhinitis, Allergic (approved 1988)

Mechanism of action

Histamine H1 receptorANTAGONIST
HRH1 antagonist
- Histamine H1 receptor (HRH1) ↗

Approval history

withdrawnJun 1, 1988

Chemistry & pharmacology

Loading structure…

SMILES

COC1=CC=C(CCN2CCC(CC2)NC3=NC4=C(C=CC=C4)N3CC5=CC=C(F)C=C5)C=C1

Mol. weight: 458.5703 g/mol
Lipinski Ro5: 1 violation(s)
Rule of 3: No
Chirality: Achiral Molecule
Inorganic: No
Polymer: No
Delivery: Oral

Oral

Yes

Parenteral

Topical

Sources

Also known as

1-(p-fluorobenzyl)-2-((1-(2-(p-methoxyphenyl)ethyl)piperid-4-yl)amino)benzimidazole
1-(p-fluorobenzyl)-2-((1-(2-(p-methoxyphenyl)ethyl)piperid-4-yl)amino)benzimidazole
1-(p-fluorobenzyl)-2-((1-(p-methoxyphenethyl)-4-piperidyl)amino)benzimidazole
1-(p-fluorobenzyl)-2-((1-(p-methoxyphenethyl)-4-piperidyl)amino)benzimidazole
astemisan
astemison
astemison
astemizol
astemizol
astemizole
astemizole
astemizole
astemizole
astemizole
astemizole
astemizole
astemizole
astemizole
astémizole
astémizole
astemizolum
astemizolum
gnf-pf-2461
gnf-pf-2461
hismanal
hismanal
hismanal
hismanal
histazol
pollon-eze
r 43 512
r 43 512
r 43 512
r 43 512
r 43 512
r 43 512
r-43512
r-43512

Organizations

Marketing (1)

Organization	Org type	Relationship	Date
Johnson and Johnson	For profit	NDA	Jun 1, 1977