Product Name

Alcaftadine

CAS Number

147084-10-4

LGM Pharma is an API distributor. LGM Pharma supplies APIs as per CGMP with DMF support, subject to availability and manufacturer requirements. LGM Pharma does not sell or supply APIs or finished dosage products to individual patients, doctors, or pharmacies.

Questions? Call our customer API support number 1-(800)-881-8210

Product Name:
Alcaftadine
CAS Number:
147084-10-4
Indication:
For the prevention of itching associated with allergic conjunctivitis.
Mode of Action:

Alcaftadine is a H1 histamine receptor antagonist and inhibitor of the release of histamine from mast cells. Decreased chemotaxis and inhibition of eosinophil activation has also been demonstrated.

Pharmacodynamics:

Following bilateral topical ocular administration of alcaftadine ophthalmic solution, 0.25%, the mean plasma Cmax of alcaftadine was approximately 60 pg/mL and the median Tmax occurred at 15 minutes. Plasma concentrations of alcaftadine were below the lower limit of quantification (10 pg/mL) by 3 hours after dosing. The mean Cmax of the active carboxylic acid metabolite was approximately 3 ng/mL and occurred at 1 hour after dosing. Plasma concentrations of the carboxylic acid metabolite were below the lower limit of quantification (100 pg/mL) by 12 hours after dosing.

Metabolism:

The metabolism of alcaftadine is mediated by non-CYP450 cytosolic enzymes to the active carboxylic acid metabolite.

IUPAC:
5H-Imidazo(2, 1-b)(3)benzazepine-3-carboxaldehyde, 6, 11-dihydro-11-(1-methyl-4- piperidinylidene)-
ATC:
S01GX11
PubChem:
19371515
DrugBank:
DB06766
Formula:
C19-H21-N3-O
Molecular Mass:
307.3949
Synonyms:
Alcaftadine, Lastacaft, R 89674, R89674, UNII-7Z8O94ECSX
SMILES:
C1(=C2CCN(CC2)C)c2c(CCn3c1ncc3C=O)cccc2
InChi:
1S/C19H21N3O/c1-21-9-6-15(7-10-21)18-17-5-3-2-4-14(17)8-11-22-16(13-23)12-20-19(18)22/h2-5,12-13H,6-11H2,1H3
General Reference:
General Reference:

 

  1. Mahvan TD, Buckley WA, Hornecker JR: Alcaftadine for the prevention of itching associated with allergic conjunctivitis. Ann Pharmacother. 2012 Jul-Aug;46(7-8):1025-32. doi: 10.1345/aph.1Q755. Epub 2012 Jul 17. Pubmed
  2. Simons FE, Simons KJ: Histamine and H1-antihistamines: celebrating a century of progress. J Allergy Clin Immunol. 2011 Dec;128(6):1139-1150.e4. doi: 10.1016/j.jaci.2011.09.005. Epub 2011 Oct 27. Pubmed
  3. Hussar DA, Samuel J: Vilazodone hydrochloride, linagliptin, and alcaftadine. J Am Pharm Assoc (2003). 2011 Jul-Aug;51(4):557-9. doi: 10.1331/JAPhA.2011.11534. Pubmed
  4. of a

Products currently covered by valid US Patents are offered for R&D use in accordance with 35 USC 271(e)+A13(1). Any patent infringement and resulting liability is solely at buyer risk.

LGM currently offers Monoclonal Antibodies (mAbs) for non-GMP/R&D use. Please inquire about Monoclonal Antibodies produced under GMP conditions.

Questions? Call our customer API support number 1-(800)-881-8210. 

Ask us about this product

API’s From Quality Manufacturers:

  • Streamlined API supply towards initial research stages as well as larger quantities of cGMP material for clinical trials and product commercialization
  • Premium quality GMP certified and fully accredited API manufacturing plants
  • Technical packages as well as access to filed DMF, ASMF or CEP (subject to availability)
  • Regulatory and technical assistance towards any submission type based on specific customer requirements

Find an API Product

Search
Generic filters