Inxight Drugs

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

National Institutes of Health Divider Arrow

NCATS

Return Home Inxight Drugs

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

Show Filters

Hide Filters

Development Status

US Approved Rx

2

Other

1

All Match

Any Match

Exclude Selected

Exclude Selected

Primary Target

Cytidine deaminase

2

RNA

2

Thymidylate synthase

2

All Match

Any Match

Exclude Selected

Exclude Selected

Highest Phase

Approved

2

All Match

Any Match

Exclude Selected

Exclude Selected

Approval Year

1998

2

Unknown

1

All Match

Any Match

Exclude Selected

Exclude Selected

Condition

Breast cancer

2

Colorectal cancer

2

All Match

Any Match

Exclude Selected

Exclude Selected

Treatment Modality

Primary

2

All Match

Any Match

Exclude Selected

Exclude Selected

CNS Activity

CNS Penetrant

2

All Match

Any Match

Exclude Selected

Exclude Selected

Originator

Hoffman-La Roche

2

All Match

Any Match

Exclude Selected

Exclude Selected

Substance Class

Chemical

3

All Match

Any Match

Exclude Selected

Exclude Selected

Code System

CAS

3

EPA CompTox

3

FDA UNII

3

PUBCHEM

3

CHEBI

2

All Match

Any Match

Exclude Selected

Exclude Selected

ATC Level 1

ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

1

All Match

Any Match

Exclude Selected

Exclude Selected

ATC Level 2

ANTINEOPLASTIC AGENTS

1

All Match

Any Match

Exclude Selected

Exclude Selected

ATC Level 3

ANTIMETABOLITES

1

All Match

Any Match

Exclude Selected

Exclude Selected

ATC Level 4

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

5'-DEOXY-5-FLUOROCYTIDINE

8RWB05I6ON

Export Data
Search for Structure

Status:

US Approved Rx (2018)

First approved in 1998

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Thymidylate synthase

Cytidine deaminase

Conditions:

Colorectal cancer

Capecitabine is a fluoropyrimidine carbamate with antineoplastic activity. It is an orally administered systemic prodrug which is converted to 5-fluorouracil (5-FU). Both normal and tumor cells metabolize 5-FU to 5-fluoro-2’-deoxyuridine monophosphat...

e (FdUMP) and 5-fluorouridine triphosphate (FUTP). These metabolites cause cell injury by two different mechanisms. First, FdUMP and the folate cofactor, N5-10-methylenetetrahydrofolate, bind to thymidylate synthase (TS) to form a covalently bound ternary complex. This binding inhibits the formation of thymidylate from 2’-deoxyuridylate. Thymidylate is the necessary precursor of thymidine triphosphate, which is essential for the synthesis of DNA, so that a deficiency of this compound can inhibit cell division. Second, nuclear transcriptional enzymes can mistakenly incorporate FUTP in place of uridine triphosphate (UTP) during the synthesis of RNA. This metabolic error can interfere with RNA processing and protein synthesis. Most common adverse reactions (≥30%) were diarrhea, hand-and-foot syndrome, nausea, vomiting, abdominal pain, fatigue/weakness, and hyperbilirubinemia. The concentration of 5-fluorouracil is increased and its toxicity may be enhanced by leucovorin.

2',3'-DI-O-ACETYL-5'-DEOXY-5-FLUOROCYTIDINE

Q6KTK8KQR2

Export Data
Search for Structure

Status:

Other

Class (Stereo):

CHEMICAL (ABSOLUTE)

CAPECITABINE

6804DJ8Z9U

Export Data
Search for Structure

Status:

US Approved Rx (2018)

First approved in 1998

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Thymidylate synthase

Cytidine deaminase

Conditions:

Colorectal cancer

Capecitabine is a fluoropyrimidine carbamate with antineoplastic activity. It is an orally administered systemic prodrug which is converted to 5-fluorouracil (5-FU). Both normal and tumor cells metabolize 5-FU to 5-fluoro-2’-deoxyuridine monophosphat...

e (FdUMP) and 5-fluorouridine triphosphate (FUTP). These metabolites cause cell injury by two different mechanisms. First, FdUMP and the folate cofactor, N5-10-methylenetetrahydrofolate, bind to thymidylate synthase (TS) to form a covalently bound ternary complex. This binding inhibits the formation of thymidylate from 2’-deoxyuridylate. Thymidylate is the necessary precursor of thymidine triphosphate, which is essential for the synthesis of DNA, so that a deficiency of this compound can inhibit cell division. Second, nuclear transcriptional enzymes can mistakenly incorporate FUTP in place of uridine triphosphate (UTP) during the synthesis of RNA. This metabolic error can interfere with RNA processing and protein synthesis. Most common adverse reactions (≥30%) were diarrhea, hand-and-foot syndrome, nausea, vomiting, abdominal pain, fatigue/weakness, and hyperbilirubinemia. The concentration of 5-fluorouracil is increased and its toxicity may be enhanced by leucovorin.

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