PARP-1 And PARP-2 Inhibitor Niraparib（MK-4827）

Buy PARP-1 And PARP-2 Inhibitor Niraparib（MK-4827）CAS No.: 1038915-60-4

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Niraparib (trade name Zejula) is an orally active small molecule PARP inhibitor developed by Tesaro to treat ovarian cancer.

Niraparib was granted fast track designation by the US Food and Drug Administration (FDA), and Tesaro submitted a new drug application in 2016. It was approved on 27 March 2017 in the US,but is not approved in Europe as of June 2017.

CAS No.: 1038915-60-4
Other Names: Niraparib
MF: C19H20N4O
EINECS No.: 1038915-60-4
Place of Origin: Shanghai, China (Mainland)
Type: Antineoplastic Agents
Grade Standard: Medicine Grade
Usage: Animal Pharmaceuticals
Brand Name: TwoChem
Model Number: API
Purity: 99%
Name: Niraparib
Appearance: Off-White Powder
Grade: Phamaceutical Grade

Application: Active Pharmaceutical Ingredients
Niraparib (MK-4827), a new, potent andorally available PARP-1 and PARP-2 inhibitor, is currently in phase IIIclinical trials for the treatment of ovarian cancer and phase III trials areplanned to begin for breast cancer.
The drug is used in form of the salt niraparib tosylate monohydrate, which is white to off-white, non-hygroscopic crystals

Medical uses
The drug is approved by the US FDA for the maintenance treatment of adult patients with recurrent epithelial ovarian, fallopian tube, or primary peritoneal cancer who are in complete or partial response to platinum-based chemotherapy.

In a study with 553 patients, progression-free survival (PFS) for patients with a deleterious or suspected deleterious BRCA mutation in the germline was 21.0 months under niraparib therapy, as compared to 5.5 months under placebo. Patients without such a mutation had a PFS of 9.3 months under niraparib versus 3.9 months under placebo.

Side effects
The most common side effects in studies were low blood cell counts, namely thrombocytopenia (in 61% of patients, severe in 29%), anemia (in 50%, severe in 25%) and neutropenia (in 30%, severe in 20%). Other, mostly mild to moderate side effects included nausea, fatigue, and constipation. In a study running over 250 days (median), 15% of patients had to permanently discontinue niraparib due to adverse effects.