Inxight Drugs

U.S. Department of Health & Human Services Divider Arrow

National Institutes of Health Divider Arrow

NCATS

This repository is under review for potential modification in compliance with Administration directives.

Return Home Inxight Drugs

Home
Browse Drugs
Search
- Structure Search
- Sequence Search
Downloads
About

Show Filters

Hide Filters

Development Status

US Approved Rx

2

All Match

Any Match

Exclude Selected

Exclude Selected

Primary Target

FK506-binding protein 1A

2

All Match

Any Match

Exclude Selected

Exclude Selected

Highest Phase

Approved

2

All Match

Any Match

Exclude Selected

Exclude Selected

Approval Year

2001

2

All Match

Any Match

Exclude Selected

Exclude Selected

Condition

Atopic dermatitis

2

All Match

Any Match

Exclude Selected

Exclude Selected

Treatment Modality

Palliative

2

All Match

Any Match

Exclude Selected

Exclude Selected

Originator

Novatris

2

All Match

Any Match

Exclude Selected

Exclude Selected

Substance Class

Chemical

2

All Match

Any Match

Exclude Selected

Exclude Selected

Code System

CAS

2

FDA UNII

2

PUBCHEM

2

SMS_ID

2

ChEMBL

1

All Match

Any Match

Exclude Selected

Exclude Selected

ATC Level 1

DERMATOLOGICALS

1

All Match

Any Match

Exclude Selected

Exclude Selected

ATC Level 2

OTHER DERMATOLOGICAL PREPARATIONS

1

All Match

Any Match

Exclude Selected

Exclude Selected

ATC Level 3

OTHER DERMATOLOGICAL PREPARATIONS

1

All Match

Any Match

Exclude Selected

Exclude Selected

ATC Level 4

Agents for atopic dermatitis, excluding corticosteroids

1

All Match

Any Match

Exclude Selected

Exclude Selected

Substance Form

Principal Form

1

Salts, Hydrates, Esters, etc.

1

All Match

Any Match

Exclude Selected

Exclude Selected

Showing 1 - 2 of 2 results

First page disabled
Previous page disabled
1
Next page disabled
Next page disabled

PIMECROLIMUS

7KYV510875

Export Data
Search for Structure

Status:

US Approved Rx (2019)

First approved in 2001

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

FK506-binding protein 1A

Conditions:

Atopic dermatitis

Pimecrolimus, an ascomycin macrolactam derivative, is an inhibitor of T-cell and mast-cell activation, developed and launched by Novartis for the potential treatment of psoriasis and allergic, irritant and atopic dermatitis. The topical formulation h...

ad been launched in the US by February 2002 for mild-to-moderate atopic dermatitis in patients aged two years and older. Pimecrolimus is an immunomodulating agent. The mechanism of action of pimecrolimus in atopic dermatitis is not known. While the following have been observed, the clinical significance of these observations in atopic dermatitis is not known. It has been demonstrated that pimecrolimus binds with high affinity to macrophilin-12 (FKBP-12) and inhibits the calcium dependent phosphatase, calcineurin. Therefore, it inhibits T cell activation by blocking the transcription of early cytokines. In particular, pimecrolimus inhibits at nanomolar concentrations Interleukin-2 and interferon gamma (Th1-type) and Interleukin-4 and Interleukin-10 (Th2-type) cytokine synthesis in human T-cells. In addition, pimecrolimus prevents the release of inflammatory cytokines and mediators from mast cells in vitro after stimulation by antigen/IgE. Following the administration of a single oral radiolabeled dose of pimecrolimus numerous circulating O-demethylation metabolites were seen. Studies with human liver microsomes indicate that pimecrolimus is metabolized in vitro by the CYP3A sub-family of metabolizing enzymes. No evidence of skin mediated drug metabolism was identified in vivo using the minipig or in vitro using stripped human skin.

PIMECROLIMUS HYDRATE

89GTE436P6

Export Data
Search for Structure

Status:

US Approved Rx (2019)

First approved in 2001

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

FK506-binding protein 1A

Conditions:

Atopic dermatitis

Pimecrolimus, an ascomycin macrolactam derivative, is an inhibitor of T-cell and mast-cell activation, developed and launched by Novartis for the potential treatment of psoriasis and allergic, irritant and atopic dermatitis. The topical formulation h...

ad been launched in the US by February 2002 for mild-to-moderate atopic dermatitis in patients aged two years and older. Pimecrolimus is an immunomodulating agent. The mechanism of action of pimecrolimus in atopic dermatitis is not known. While the following have been observed, the clinical significance of these observations in atopic dermatitis is not known. It has been demonstrated that pimecrolimus binds with high affinity to macrophilin-12 (FKBP-12) and inhibits the calcium dependent phosphatase, calcineurin. Therefore, it inhibits T cell activation by blocking the transcription of early cytokines. In particular, pimecrolimus inhibits at nanomolar concentrations Interleukin-2 and interferon gamma (Th1-type) and Interleukin-4 and Interleukin-10 (Th2-type) cytokine synthesis in human T-cells. In addition, pimecrolimus prevents the release of inflammatory cytokines and mediators from mast cells in vitro after stimulation by antigen/IgE. Following the administration of a single oral radiolabeled dose of pimecrolimus numerous circulating O-demethylation metabolites were seen. Studies with human liver microsomes indicate that pimecrolimus is metabolized in vitro by the CYP3A sub-family of metabolizing enzymes. No evidence of skin mediated drug metabolism was identified in vivo using the minipig or in vitro using stripped human skin.

HHS VULNERABILITY DISCLOSURE

For language access assistance, contact the NCATS Public Information Officer

National Center for Advancing Translational Sciences (NCATS),
6701 Democracy Boulevard, Bethesda MD 20892-4874 • 301-594-8966


			version 1.1