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

Primary Target

CAKI-1

3

Histamine H1 receptor

316

Dopamine D2 receptor

311

DNA

282

Serotonin 2a (5-HT2a) receptor

237

All Match

Any Match

Exclude Selected

Exclude Selected

Development Status

US Approved Rx

3

All Match

Any Match

Exclude Selected

Exclude Selected

Highest Phase

Approved

3

All Match

Any Match

Exclude Selected

Exclude Selected

Approval Year

1996

2

2007

1

All Match

Any Match

Exclude Selected

Exclude Selected

Condition

Advanced ovarian cancer

2

Metastatic breast cancer

2

Non-small cell lung cancer

2

Pancreatic cancer

2

Advanced renal cell carcinoma

1

All Match

Any Match

Exclude Selected

Exclude Selected

Treatment Modality

Primary

3

All Match

Any Match

Exclude Selected

Exclude Selected

CNS Activity

CNS Penetrant

2

All Match

Any Match

Exclude Selected

Exclude Selected

Originator

Eli Lilly|University of Innsbruck

2

Wyeth

1

All Match

Any Match

Exclude Selected

Exclude Selected

Substance Class

Chemical

3

All Match

Any Match

Exclude Selected

Exclude Selected

Code System

CAS

3

ChEMBL

3

DAILYMED

3

DRUG BANK

3

EPA CompTox

3

All Match

Any Match

Exclude Selected

Exclude Selected

ATC Level 1

ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

2

All Match

Any Match

Exclude Selected

Exclude Selected

ATC Level 2

ANTINEOPLASTIC AGENTS

2

All Match

Any Match

Exclude Selected

Exclude Selected

ATC Level 3

ANTIMETABOLITES

1

OTHER ANTINEOPLASTIC AGENTS

1

All Match

Any Match

Exclude Selected

Exclude Selected

ATC Level 4

Protein kinase inhibitors

1

Pyrimidine analogues

1

All Match

Any Match

Exclude Selected

Exclude Selected

Substance Form

Principal Form

2

Salts, Hydrates, Esters, etc.

1

All Match

Any Match

Exclude Selected

Exclude Selected

Showing 1 - 3 of 3 results

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

TEMSIROLIMUS

624KN6GM2T

Export Data
Search for Structure

Status:

US Approved Rx (2018)

First approved in 2007

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Serine/threonine-protein kinase mTOR

Conditions:

Advanced renal cell carcinoma

Temsirolimus is an intravenous drug for the treatment of renal cell carcinoma (RCC), developed by Wyeth Pharmaceuticals and approved by the FDA in late May 2007, and was also approved by the European Medicines Agency (EMEA) on November 2007. It is a ...

derivative of sirolimus and is sold as Torisel. Temsirolimus is an inhibitor of mTOR (mammalian target of rapamycin). Temsirolimus binds to an intracellular protein (FKBP-12), and the protein-drug complex inhibits the activity of mTOR that controls cell division. Inhibition of mTOR activity resulted in a G1 growth arrest in treated tumor cells. When mTOR was inhibited, its ability to phosphorylate p70S6k and S6 ribosomal protein, which are downstream of mTOR in the PI3 kinase/AKT pathway was blocked. In in vitro studies using renal cell carcinoma cell lines, temsirolimus inhibited the activity of mTOR and resulted in reduced levels of the hypoxia-inducible factors HIF-1 and HIF-2 alpha, and the vascular endothelial growth factor.

GEMCITABINE HYDROCHLORIDE

U347PV74IL

Export Data
Search for Structure

Status:

US Approved Rx (2011)

First approved in 1996

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Ribonucleoside-diphosphate reductase M1 chain

Conditions:

Advanced ovarian cancer

Metastatic breast cancer

Pancreatic cancer

Non-small cell lung cancer

Gemcitabine is a nucleoside analog used as chemotherapy. It is marketed as Gemzar® by Eli Lilly and Company. Gemcitabine inhibits thymidylate synthetase, leading to inhibition of DNA synthesis and cell death. Gemcitabine is a prodrug so activity occu...

rs as a result of intracellular conversion to two active metabolites, gemcitabine diphosphate and gemcitabine triphosphate by deoxycitidine kinase. Gemcitabine diphosphate also inhibits ribonucleotide reductase, the enzyme responsible for catalyzing synthesis of deoxynucleoside triphosphates required for DNA synthesis. Finally, Gemcitabine triphosphate (diflurorodeoxycytidine triphosphate) competes with endogenous deoxynucleoside triphosphates for incorporation into DNA. Gemcitabine is indicated for the treatment of advanced ovarian cancer that has relapsed at least 6 months after completion of platinum-based therapy; metastatic ovarian cancer; inoperable, locally advanced (Stage IIIA or IIIB), or metastatic (Stage IV) non-small cell lung cancer; and locally advanced (nonresectable Stage II or Stage III) or metastatic (Stage IV) adenocarcinoma of the pancreas.

GEMCITABINE

B76N6SBZ8R

Export Data
Search for Structure

Status:

US Approved Rx (2011)

First approved in 1996

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Ribonucleoside-diphosphate reductase M1 chain

Conditions:

Advanced ovarian cancer

Metastatic breast cancer

Pancreatic cancer

Non-small cell lung cancer

Gemcitabine is a nucleoside analog used as chemotherapy. It is marketed as Gemzar® by Eli Lilly and Company. Gemcitabine inhibits thymidylate synthetase, leading to inhibition of DNA synthesis and cell death. Gemcitabine is a prodrug so activity occu...

rs as a result of intracellular conversion to two active metabolites, gemcitabine diphosphate and gemcitabine triphosphate by deoxycitidine kinase. Gemcitabine diphosphate also inhibits ribonucleotide reductase, the enzyme responsible for catalyzing synthesis of deoxynucleoside triphosphates required for DNA synthesis. Finally, Gemcitabine triphosphate (diflurorodeoxycytidine triphosphate) competes with endogenous deoxynucleoside triphosphates for incorporation into DNA. Gemcitabine is indicated for the treatment of advanced ovarian cancer that has relapsed at least 6 months after completion of platinum-based therapy; metastatic ovarian cancer; inoperable, locally advanced (Stage IIIA or IIIB), or metastatic (Stage IV) non-small cell lung cancer; and locally advanced (nonresectable Stage II or Stage III) or metastatic (Stage IV) adenocarcinoma of the pancreas.

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