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Ritlecitinib

Ritlecitinib structure

CAS No:
1792180-81-4
Formula:
C15H19N5O
Chemical Name:
Ritlecitinib
Synonyms:
1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one;1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2;PF-06651600;PF 06651600;PF06651600;1-[(2S,5R)-2-methyl-5(7H-pyrrolo[2,3-d]pyrimidine-4-ylamino)-1-piperidinly]-2-propen-1-one malonate,PF06651600;Ritlecitinib;2-Propen-1-one, 1-[(2S,5R)-2-methyl-5-(7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-1-piperidinyl]-;1-[(2S,5R)-2-Methyl-5-(7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-1-piperidinyl]-2-propen-1-one;Ritlecitinib (PF-06651600)
Categories:
Pharmaceutical Intermediates > Bulk Drug Intermediates

Description

PF-06651600 is under investigation in clinical trial NCT02974868 (Study To Evaluate The Efficacy And Safety Profile Of PF-06651600 And PF-06700841 In Subjects With Alopecia Areata).|Ritlecitinib is an orally available small-molecule inhibitor of tyrosine-protein kinase JAK3 (Janus kinase 3; JAK3) with potential immunomodulatory and anti-inflammatory activities. Upon administration, ritlecitinib selectively and irreversibly binds to JAK3 and prevents the activation of the JAK-signal transducers and activators of transcription (STAT) signaling pathway. This may decrease the production of certain pro-inflammatory cytokines and prevent both an inflammatory response and the inflammation-induced damage caused by certain immunological diseases. By selectively targeting JAK3, PF-06651600 may spare interleukin (IL)-6 signaling, as well as other JAK1-dependent immunoregulatory cytokines such as IL-10, IL-27, and IL-35, which may offer a safety benefit compared to non-selective JAK inhibitors. JAK kinases are intracellular enzymes involved in signaling pathways affecting hematopoiesis, immunity and inflammation.

Ritlecitinib, a dual JAK3/TEC inhibitor, was granted FDA breakthrough status for treating alopecia areata (autoimmune-induced hair loss) in September 2018. Promising phase 3 trial results in alopecia areata were reported by Pfizer in August 2021, placing it in competition with Lilly/Incyte’s Olumiant. It is also used in clinical studies to treat vitiligo, rheumatoid arthritis, Crohn’s disease, and ulcerative colitis. Ritlecitinib achieved high JAK3 selectivity via covalent interaction with a unique cysteine residue (Cys909) in the catalytic domain.

Ritlecitinib Basic Attributes

Molecular Weight：

285.34

Exact Mass：

285.15896025

EC Number：

210-077-2

UNII：

2OYE00PC25

NCI Thesaurus Code：

C161783

Color/Form：

white to beige

Characteristics

Density：

1.272±0.06 g/cm3(Predicted)

Water Solubility：

H2O: 5mg/mL, clear (warmed)

PKA：

13.03±0.50(Predicted)

Critical Temperature & Pressure：

room temp

Safety Information

wgk germany：

WGK 3

GHS Classification：

|Warning|H361 (100%): Suspected of damaging fertility or the unborn child [Warning Reproductive toxicity]|P201, P202, P281, P308+P313, P405, and P501|The GHS information provided by 1 company from 1 notification to the ECHA C&L Inventory.

Drug Information

MeSH Entry Terms：

1-(5-((7H-pyrrolo(2,3-d)pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one

Ritlecitinib Use and Manufacturing

Looking at the history of alopecia areata drug development, ritlecitinib is the second mature drug for treating alopecia areata. It is a kinase inhibitor. Unlike the first drug, Olumiant, ritlecitinib is approved not only for adult patients but also for adolescents aged 12 and above.

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cas 1792180-81-4 1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one

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