1208319-27-0 Usage
Description
Oclacitinib Maleate (PF-03394197), also known as APOQUEL, is the first selective Janus kinase (JAK) inhibitor developed specifically for dogs. It is a pharmaceutical compound that plays a crucial role in cytokine signaling and is involved in the signal transduction of various pro-inflammatory, pro-allergic, and pruritogenic cytokines, including IL-2, IL-4, IL-6, IL-13, and IL-31, which are implicated in allergic conditions.
Uses
Used in Veterinary Medicine:
Oclacitinib Maleate (PF-03394197) is used as a therapeutic agent for the treatment of atopic dermatitis and itchiness (pruritus) caused by allergies in dogs. It effectively reduces the itchiness and dermatitis caused by flea infestations and is considered highly effective and safe for short-term use.
Used in Allergic Dermatitis Treatment:
Oclacitinib Maleate (PF-03394197) is used as a JAK inhibitor for the control of pruritus associated with allergic dermatitis in dogs. It helps break the vicious cycle of itch that exacerbates skin lesions and amplifies defects in the skin barrier function in clinically affected dogs.
Used in Atopic Dermatitis Management:
Oclacitinib Maleate (PF-03394197) is used as a JAK inhibitor for the control of atopic dermatitis in dogs at least 12 months of age. Its efficacy in managing itchiness and dermatitis is comparable to prednisolone in the short term, and it has been found to have a faster onset and cause fewer gastrointestinal issues than cyclosporine.
While Oclacitinib Maleate (PF-03394197) has been established as safe for short-term use, its long-term safety is still unknown. Some experts suggest it is best for acute flares of itchiness, while others claim it is also useful in chronic atopic dermatitis management.
Pharmacokinetics
The pharmacokinetics of oclacitinib maleate was evaluated in four separate
studies. The absolute bioavailability study used a crossover design with 10
dogs. The effect of food on bioavailability was investigated in a crossover
study with 18 dogs. The breed effect on pharmacokinetics was assessed in a
crossover study in beagles and mongrels dogs. Dose proportionality and multiple dose pharmacokinetics were evaluated in a parallel design study with
eight dogs per group. In all four studies, serial blood samples for plasma were
collected. Oclacitinib maleate was rapidly and well absorbed following oral
administration, with a time to peak plasma concentration of<1 h and an
absolute bioavailability of 89%. The prandial state of dogs did not significantly affect the rate or extent of absorption of oclacitinib maleate when
dosed orally, as demonstrated by the lack of significant differences in pharmacokinetic parameters between the oral fasted and oral fed treatment groups.
The pharmacokinetics of oclacitinib in laboratory populations of beagles and
mixed breed dogs also appeared similar. Following oral administration, the
exposure of oclacitinib maleate increased dose proportionally from 0.6 to
3.0 mg/kg. Additionally, across the pharmacokinetic studies, there were no
apparent differences in oclacitinib pharmacokinetics attributable to sex
Side effects
There are several caveats to the use of Oclacitinib maleate.
This medication is meant to control the symptoms of itching. For many patients, ending itching also ends scratching and chewing. Ending scratching and chewing ends infections and a vicious cycle can finally be broken. The problem is that while oclacitinb maleate can control itching, it does may not control the disease that is causing the itching. If there is an infection present, it will continue to be present; it simply will not be itchy. It is important not to let skin disease persist simply because the dog is comfortable. The disease must be controlled as well.
The oclacitinib maleate label contains a caution against use in patients with cancer. While oclacitinib maleate does not cause cancer, there is question about whether it can interfere with natural protective mechanisms that help control cancer. If a patient is known to have cancer or known to have an undefined growth on its body or if there is any reason to suspect a patient might be harboring cancer, it is important to discuss this caution with one's veterinarian before use of this medication.
Oclacitinib maleate appears to promote or support Demodex skin mites. It should not be used to control itching associated with Demodectic Mange.
Check Digit Verification of cas no
The CAS Registry Mumber 1208319-27-0 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,2,0,8,3,1 and 9 respectively; the second part has 2 digits, 2 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 1208319-27:
(9*1)+(8*2)+(7*0)+(6*8)+(5*3)+(4*1)+(3*9)+(2*2)+(1*7)=130
130 % 10 = 0
So 1208319-27-0 is a valid CAS Registry Number.
1208319-27-0Relevant articles and documents
Preparation method of 7H-pyrrolo [2, 3-d] pyrimidine compound
-
, (2021/01/30)
The invention discloses a preparation method of a 7H-pyrrolo [2, 3-d] pyrimidine compound. The full name of the 7H-pyrrolo [2, 3-d] pyrimidine compound is trans-N-methyl-4-(methyl-7H-pyrrolo [2, 3-d]pyrimidine-4-yl amino) cyclohexylmethanesulfonamide male
SOLID STATE FORMS OF OCLACITINIB MALEATE
-
Page/Page column 13-14, (2020/08/22)
The present invention relates to solid state forms of oclacitinib maleate and methods for the preparation of the solid state forms of oclacitinib maleate. The solid state forms of oclacitinib maleate of the present invention include amorphous oclacitinib maleate, crystalline tetramethyl urea solvate form of oclacitinib maleate, crystalline monohydrate form of oclacitinib maleate and crystalline form of oclacitinib maleate (form B).
PROCESS FOR PREPARING 7H-PYRROLO[2,3-D]PYRIMIDINE COMPOUNDS
-
, (2017/09/02)
Described herein are improved processes for the preparation of the 7H-pyrrolo[2,3-d]pyrimidine compound, N-methyl-1-{trans-4-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclohexyl}-methanesulfonamide, intermediates thereof, and veterinary acceptable salts thereof.
