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

Primary Target

Leukemia cells

2

Histamine H1 receptor

315

Dopamine D2 receptor

297

DNA

278

Bacterial penicillin-binding protein

233

All Match

Any Match

Exclude Selected

Exclude Selected

Development Status

US Previously Marketed

2

All Match

Any Match

Exclude Selected

Exclude Selected

Highest Phase

Approved

2

All Match

Any Match

Exclude Selected

Exclude Selected

Approval Year

1966

2

All Match

Any Match

Exclude Selected

Exclude Selected

Condition

Acute non-lymphocytic leukemia

2

All Match

Any Match

Exclude Selected

Exclude Selected

Treatment Modality

Primary

2

All Match

Any Match

Exclude Selected

Exclude Selected

CNS Activity

CNS Non-penetrant

2

All Match

Any Match

Exclude Selected

Exclude Selected

Originator

Burroughs Wellcome Fund

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

CHEBI

2

ChEMBL

2

DAILYMED

2

EPA CompTox

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

Purine analogues

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

THIOGUANINE ANHYDROUS

WIX31ZPX66

Export Data
Search for Structure

Status:

US Previously Marketed

First approved in 1966

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Inosine-5'-monophosphate dehydrogenase (IMPDH)

Conditions:

Acute non-lymphocytic leukemia

Thioguanine is an antineoplastic anti-metabolite used in the treatment of several forms of leukemia including acute nonlymphocytic leukemia. Anti-metabolites masquerade as purine or pyrimidine - which become the building blocks of DNA. They prevent t...

hese substances becoming incorporated in to DNA during the "S" phase (of the cell cycle), stopping normal development and division. Thioguanine was first synthesized and entered into clinical trial more than 30 years ago. It is a 6-thiopurine analogue of the naturally occurring purine bases hypoxanthine and guanine. Intracellular activation results in incorporation into DNA as a false purine base. An additional cytotoxic effect is related to its incorporation into RNA. Thioguanine is cross-resistant with mercaptopurine. Cytotoxicity is cell cycle phase-specific (S-phase). Thioguanine competes with hypoxanthine and guanine for the enzyme hypoxanthine-guanine phosphoribosyltransferase (HGPRTase) and is itself converted to 6-thioguanilyic acid (TGMP), which reaches high intracellular concentrations at therapeutic doses. TGMP interferes with the synthesis of guanine nucleotides by its inhibition of purine biosynthesis by pseudofeedback inhibition of glutamine-5-phosphoribosylpyrophosphate amidotransferase, the first enzyme unique to the de novo pathway of purine ribonucleotide synthesis. TGMP also inhibits the conversion of inosinic acid (IMP) to xanthylic acid (XMP) by competition for the enzyme IMP dehydrogenase. Thioguanine nucleotides are incorporated into both the DNA and the RNA by phosphodiester linkages, and some studies have shown that incorporation of such false bases contributes to the cytotoxicity of thioguanine. Its tumor inhibitory properties may be due to one or more of its effects on feedback inhibition of de novo purine synthesis; inhibition of purine nucleotide interconversions; or incorporation into the DNA and RNA. The overall result of its action is a sequential blockade of the utilization and synthesis of the purine nucleotides. Thioguanine is used for remission induction and remission consolidation treatment of acute nonlymphocytic leukemias. It is marketed under the trade name Lanvis and Tabloid among others.

THIOGUANINE

FTK8U1GZNX

Export Data
Search for Structure

Status:

US Previously Marketed

First approved in 1966

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Inosine-5'-monophosphate dehydrogenase (IMPDH)

Conditions:

Acute non-lymphocytic leukemia

Thioguanine is an antineoplastic anti-metabolite used in the treatment of several forms of leukemia including acute nonlymphocytic leukemia. Anti-metabolites masquerade as purine or pyrimidine - which become the building blocks of DNA. They prevent t...

hese substances becoming incorporated in to DNA during the "S" phase (of the cell cycle), stopping normal development and division. Thioguanine was first synthesized and entered into clinical trial more than 30 years ago. It is a 6-thiopurine analogue of the naturally occurring purine bases hypoxanthine and guanine. Intracellular activation results in incorporation into DNA as a false purine base. An additional cytotoxic effect is related to its incorporation into RNA. Thioguanine is cross-resistant with mercaptopurine. Cytotoxicity is cell cycle phase-specific (S-phase). Thioguanine competes with hypoxanthine and guanine for the enzyme hypoxanthine-guanine phosphoribosyltransferase (HGPRTase) and is itself converted to 6-thioguanilyic acid (TGMP), which reaches high intracellular concentrations at therapeutic doses. TGMP interferes with the synthesis of guanine nucleotides by its inhibition of purine biosynthesis by pseudofeedback inhibition of glutamine-5-phosphoribosylpyrophosphate amidotransferase, the first enzyme unique to the de novo pathway of purine ribonucleotide synthesis. TGMP also inhibits the conversion of inosinic acid (IMP) to xanthylic acid (XMP) by competition for the enzyme IMP dehydrogenase. Thioguanine nucleotides are incorporated into both the DNA and the RNA by phosphodiester linkages, and some studies have shown that incorporation of such false bases contributes to the cytotoxicity of thioguanine. Its tumor inhibitory properties may be due to one or more of its effects on feedback inhibition of de novo purine synthesis; inhibition of purine nucleotide interconversions; or incorporation into the DNA and RNA. The overall result of its action is a sequential blockade of the utilization and synthesis of the purine nucleotides. Thioguanine is used for remission induction and remission consolidation treatment of acute nonlymphocytic leukemias. It is marketed under the trade name Lanvis and Tabloid among others.

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