Nepafenac

  • #LGM Pharma is a Nepafenac CAS# 78281-72-8 API supplier distributor based in the USA. Inquire about DMF, cGMP, price, availability, delivery, purity, and more.
  • #Questions? Call our customer API support number 1-(800)-881-8210.
  • #LGM Pharma offers this active ingredient but not the finished dosage forms.

Product Details:

  • CAS No: 78281-72-8
  • AHFC code:
  • Synonyms: 2-(2-Amino-3-benzoylphenyl)acetamide, 2-Amino-3-benzoylbenzeneacetamide, AHR 9434, AHR-9434, AL 6515, AL-6515, Ilevro, Nepafenac, Nevanac, UNII-0J9L7J6V8C
  • ATC Code: S01BC10
  • Chemical Formula: C15-H14-N2-O2
  • Molecular Weight: 254.288
  • Assay/Purity: Typically NLT 98%
  • DrugBank: DB06802
  • SMILES: c1ccc(C(=O)c2c(c(ccc2)CC(N)=O)N)cc1
  • InChl: 1S/C15H14N2O2/c16-13(18)9-11-7-4-8-12(14(11)17)15(19)10-5-2-1-3-6-10/h1-8H,9,17H2,(H2,16,18)
  • PubChem: 151075
  • IUPAC: Benzeneacetamide, 2-amino-3-benzoyl-

Additional Details

Indication:
For the treatment of pain and inflammation associated with cataract surgery.
Pharmacodynamics:
Low but quantifiable plasma concentrations of nepafenac and amfenac were observed in the majority of subjects 2 and 3 hours postdose, respectively, following bilateral topical ocular TID dosing of nepafenac ophthalmic suspension, 0.1%. The mean steady-state Cmax for nepafenac and for amfenac were 0.310 ± 0.104 ng/ml and 0.422 ± 0.121 ng/ml, respectively, following ocular administration.
Mode of Action:
Nepafenac is a prodrug. After penetrating the cornea, nepafenac undergoes rapid bioactivation to amfenac, which is a potent NSAID that uniformly inhibits the COX1 and COX2 activity.
Metabolism:
Nepafenac (prodrug) is deaminated to amfenac (active compound) in the ciliary body epithelium, retina, and choroid by intraocular hydrolases. Subsequently, amfenac undergoes extensive metabolism to more polar metabolites involving hydroxylation of the aromatic ring leading to glucuronide conjugate formation.
Toxicity:
Ocularly applied non-steroidal anti-inflammatory drugs may cause increased bleeding of ocular tissues (including hyphemas) in conjunction with ocular surgery.
General Reference:
Gamache DA, Graff G, Brady MT, Spellman JM, Yanni JM: Nepafenac, a unique nonsteroidal prodrug with potential utility in the treatment of trauma-induced ocular inflammation: I. Assessment of anti-inflammatory efficacy. Inflammation. 2000 Aug;24(4):357-70. PubmedKe TL, Graff G, Spellman JM, Yanni JM: Nepafenac, a unique nonsteroidal prodrug with potential utility in the treatment of trauma-induced ocular inflammation: II. In vitro bioactivation and permeation of external ocular barriers. Inflammation. 2000 Aug;24(4):371-84. PubmedLane SS, Modi SS, Lehmann RP, Holland EJ: Nepafenac ophthalmic suspension 0.1% for the prevention and treatment of ocular inflammation associated with cataract surgery. J Cataract Refract Surg. 2007 Jan;33(1):53-8. PubmedWalters T, Raizman M, Ernest P, Gayton J, Lehmann R: In vivo pharmacokinetics and in vitro pharmacodynamics of nepafenac, amfenac, ketorolac, and bromfenac. J Cataract Refract Surg. 2007 Sep;33(9):1539-45. PubmedBucci FA Jr, Waterbury LD: Re: Pharmacokinetics and pharmacodynamics of nepafenac, amfenac, ketorolac, and bromfenac. J Cataract Refract Surg. 2008 Aug;34(8):1226; author reply 1226-7. PubmedSummary Basis of Decision (SBD): NEVANAC. Health Canada
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.

API’s From Quality Manufacturers:

  • Cost effective materials based on specific requirements
  • Small quantities for initial research and larger development quantities towards product commercialization

 

  • Technical packages, letters of access to filed DMFs
  • Complete assistance in any regulatory filings
  • Top quality GMP certified manufacturers
  • Have necessary regulatory credentials

 

Related YouTube Videos