CAS: 608141-41-9 Apremilast API/Apis C22h24n2o7s for Treating Psoriatic Arthritis

 

 

Product Name:	Apremilast (CC-10004)
Synonyms:	ApreMilast;(S)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione;(S)-N-(2-(1-(3-Ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl)-1,3-dioxoisoindolin-4-yl)acetamide;ApreMilast,CC-10004;AcetaMide, N-[2-[(1S)-1-(3-ethoxy-4-Methoxyphenyl)-2-(Methylsulfonyl)ethyl]-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]-;Appleton West;(S)-N-(2-(1-(3-Ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl)-1,3-dioxoisoindolin-4-yl)acetamide Apremilast (CC-10004;(S)-N-(2-(1-(3-Ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl)-1,3-dioxoisoindolin-4-yl)
CAS:	608141-41-9
MF:	C22H24N2O7S
Appearance:	White Powder
Product Categories:	Inhibitor;Inhibitors;Other series

 

 

Description:

Apremilast (Otezla) was approved by the FDA on March 21, 2014 for the treatment of adult patients with active psoriatic arthritis. Apremilast is a member of a new class of oral small molecule inhibitors of the phosphosphodiesterase 4 (PDE4) enzyme. When PDE4 is inhibited in immune cells, it results in elevation of intracellular cyclic adenosine monophosphate (cAMP) levels, which can regulate inflammatory mediators. The current clinical data indicate that apremilast is an effective and well tolerated option for the management of psoriasis and PsA in adults.

 

 

Uses:

Treating active psoriatic arthritis. It is also used to treat moderate to severe plaque psoriasis in certain patients.

 

 

Metabolism and Drug interaction:

Oral administration of apremilast has an absolute biovailability of 73% with peak concentration at 2.5 hours (Tmax). The half-life of apremilast is 6-9 hours. Apremilast is metabolized by the both cytochrome (CYP) and non-CYP pathways. In vitro studies have demonstrated that apremilast metabolism is primarily mediated by the CYP3A4 pathway. Thus, concomitant use of apremilast with CYP450 enzyme inducers (such as rifampin, phenobarbital, carbamazepine, phenytoin) is not recommended. There are no significant drug-drug interactions with oral contraceptives, ketoconazole, or methotrexate.

 

 

Safety information:

1.Apremilast may cause depression. The risk may be greater in patients who have a history of depression or suicidal thoughts or actions. Families and caregivers must closely watch patients who take apremilast. It is important to keep in close contact with the patient's doctor. Tell the doctor right away if the patient has new, worsened, or sudden symptoms, such as depression; anxiety, restlessness, or irritability; panic attacks; or any changes in behavior. Contact the doctor right away if any signs of suicidal thoughts or actions occur.
2.Apremilast may cause weight loss. You will need to have regular weight checks while you are taking apremilast.

 

COA:

 

Items	Specifications	Results
Appearance	Off-white and white powder	Off-white powder
Related Substances	Any single unknown impurity≤0.1% Total impurities:≤0.5%	0.09% 0.13%
Enantiomer	<0.5%	0.12%
Loss on drying	Not more than 0.5%	0.03%
Melting Point	154~158ºC	155.6~156.7ºC
Residue on ignition	Not more than 0.5%	0.01%
Residual solvents	Methanol <3000ppm Ethanol <5000ppm THF<720ppm Acetone <5000ppm	N.D. N.D. 66ppm 800ppm N.D.
Purity(HPLC)	≥99.5%	99.87%
Results	The product conforms to the above specifications

CAS: 608141-41-9 Apremilast API/Apis C22h24n2o7s for Treating Psoriatic Arthritis