OXATOMIDE

Possibly Marketed Outside US

Details

Stereochemistry	ACHIRAL
Molecular Formula	C27H30N4O
Molecular Weight	426.5533
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

O=C1NC2=CC=CC=C2N1CCCN3CCN(CC3)C(C4=CC=CC=C4)C5=CC=CC=C5

InChI

InChIKey=BAINIUMDFURPJM-UHFFFAOYSA-N

InChI=1S/C27H30N4O/c32-27-28-24-14-7-8-15-25(24)31(27)17-9-16-29-18-20-30(21-19-29)26(22-10-3-1-4-11-22)23-12-5-2-6-13-23/h1-8,10-15,26H,9,16-21H2,(H,28,32)

HIDE SMILES / InChI

Molecular Formula	C27H30N4O
Molecular Weight	426.5533
Charge	0
Count	MOL RATIO 1 MOL RATIO (average)

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description

Oxatomide is a H1-histamine receptor antagonist developed for the treatment of broad spectrum of allergic and other hypersensitivity reactions. The drug is currently marketed in Japan, Taiwan, Italy, Portugal, Indonesia, Argentina, South Africa.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Histamine H1 receptor 315	Antagonist 2,778		6.23 null [pIC50]

Conditions

Condition	Modality	Highest Phase	Product
Chronic urticaria 2	Primary	Approved 8,429	TINSET
Follicular conjunctivitis 2	Primary	Approved 8,429	TINSET
Asthma 241	Palliative	Approved 8,429	TINSET
Perennial allergic rhinitis 47	Primary	Approved 8,429	TINSET
Atopic eczema 2	Primary	Approved 8,429	TINSET
Food allergy 2	Primary	Approved 8,429	TINSET

PubMed

Show entries

Title	Date	PubMed
Inhibition of mediator release in RBL-2H3 cells by some H1-antagonist derived anti-allergic drugs: relation to lipophilicity and membrane effects.	1995 Feb	7655991
Oxatomide in the treatment of atopic dermatitis in breast-fed and very young infants.	2001 Aug	11573062
Double-blind multicenter study on the efficacy and tolerability of cetirizine compared with oxatomide in chronic idiopathic urticaria in preschool children.	2001 Jul	11476462
The role of central histaminergic neuron system as an anticonvulsive mechanism in developing brain.	2001 Nov	11701252
Gateways to clinical trials.	2002 Jan-Feb	11980386

Showing 1 to 5 of 15 entries

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Patents

Sample Use Guides

In Vivo Use Guide

Oxatomide should be taken twice daily, after breakfast and after dinner: 30 mg for adults and 0.5 mg/kg for children older tan 1 year.

Route of Administration: Oral

In Vitro Use Guide

The effect of oxatomide on the immunologic release of preformed (histamine and tryptase) and de novo synthesized mediators (leukotriene C4:LTC4 and prostaglandin D2:PGD2) from human basophils and mast cells purified (from 10 to 82%) from human lung parenchyma (HLMC) and skin tissue (HSMC) was studied in vitro. Preincubation (15 min, 37 degrees C) of basophils with oxatomide (10(-7)-10(-5) M) before Der p I antigen or anti-IgE challenge concentration-dependently (10-40%) inhibited the immunologic release of histamine and LTC4. Oxatomide (10(-7)-10(-5) M) also inhibited (10-40%) histamine, tryptase and LTC4 release from HLMC activated by anti-IgE. In addition, oxatomide caused a concentration-dependent inhibition of histamine, tryptase and PGD2 release from HSMC immunologically challenged with a monoclonal antibody against the alpha chain of the high affinity receptor for IgE (anti-Fc epsilon RI) or anti-IgE.