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Primary Target

DNA polymerase lambda

4

Histamine H1 receptor

315

Dopamine D2 receptor

297

DNA

278

Bacterial penicillin-binding protein

233

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Development Status

US Approved Rx

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Other

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Highest Phase

Approved

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Phase II

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Approval Year

1969

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Unknown

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Condition

Chronic myelogenous leukemia

3

Lymphomatous meningitis

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Acute focal cerebral ischemia

1

Cancer

1

Type 2 diabetes mellitus

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Treatment Modality

Primary

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CNS Activity

CNS Active

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Originator

University of California-Berkeley

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Wood, H.B.|Allerton, R.|Diehl, H.W.|Fletcher, H.G

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Chemical

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Code System

CAS

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EPA CompTox

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FDA UNII

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NSC

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PUBCHEM

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ATC Level 1

ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

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ANTINEOPLASTIC AGENTS

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ANTIMETABOLITES

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OTHER ANTINEOPLASTIC AGENTS

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ATC Level 4

Combinations of antineoplastic agents

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Pyrimidine analogues

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Principal Form

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Salts, Hydrates, Esters, etc.

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Showing 1 - 4 of 4 results

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CYTARABINE

04079A1RDZ

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Status:

US Approved Rx (1990)

First approved in 1969

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

DNA polymerase lambda

Conditions:

Chronic myelogenous leukemia

Lymphomatous meningitis

Cytarabine is a pyrimidine nucleoside analog. Cytarabine or cytosine arabinoside (Cytosar-U or Depocyt) is a chemotherapy agent used mainly in the treatment of cancers of white blood cells such as acute myeloid leukemia (AML) and non-Hodgkin lymphoma...

. It also has antiviral and immunosuppressant properties. Cytarabine is an antimetabolite antineoplastic agent that inhibits the synthesis of DNA. It is a cell cycle phase-specific, affecting cells only during the S phase of cell division. Intracellularly, cytarabine is converted into cytarabine-5-triphosphate (ara-CTP), which is the active metabolite. The mechanism of action is not completely understood, but it appears that ara-CTP acts primarily through inhibition of DNA polymerase. Incorporation into DNA and RNA may also contribute to cytarabine cytotoxicity. Cytarabine is cytotoxic to a wide variety of proliferating mammalian cells in culture.The drug has a short plasma half-life, low stability and limited bioavailability. Overdosing of patients with continuous infusions may lead to side effects. Thus, various prodrug strategies and delivery systems have been explored extensively to enhance the half-life, stability and delivery of cytarabine. Alternative, delivery systems of cytarabine have emerged for the treatment of different cancers. The liposomal-cytarabine formulation has been approved for the treatment of lymphomatous meningitis.

ISOSTEVIOL

091QB7QO95

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Status:

Other

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

DNA polymerase beta

DNA topoisomerase II

DNA polymerase lambda

DNA polymerase alpha subunit

Conditions:

Acute focal cerebral ischemia

Type 2 diabetes mellitus

Stevia is the common word to refer to the plant stevia rebaudiana which is the sweetest of the stevia species of plants and historically used as a sweetening agent. Several studies have suggested that in addition to their sweetness, steviosides and t...

heir related compounds, including rebaudioside A and isosteviol, may offer additional therapeutic benefits. These benefits include anti-hyperglycaemic, anti-hypertensive, anti-inflammatory, anti-tumor, anti-diarrheal, diuretic, and immunomodulatory actions. Isosteviol inhibits DNA polymerases and human DNA topoisomerase II. It also retards growth of three different types of human cancer cells and inhibits inflammation induced by TPA. Isosteviol had been in phase II clinical trials for the treatment of Type 2 diabetes mellitus.

CYTARABINE-5'-PALMITATE

TFX122G3KD

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Status:

US Approved Rx (1990)

First approved in 1969

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

DNA polymerase lambda

Conditions:

Chronic myelogenous leukemia

Lymphomatous meningitis

Cytarabine is a pyrimidine nucleoside analog. Cytarabine or cytosine arabinoside (Cytosar-U or Depocyt) is a chemotherapy agent used mainly in the treatment of cancers of white blood cells such as acute myeloid leukemia (AML) and non-Hodgkin lymphoma...

. It also has antiviral and immunosuppressant properties. Cytarabine is an antimetabolite antineoplastic agent that inhibits the synthesis of DNA. It is a cell cycle phase-specific, affecting cells only during the S phase of cell division. Intracellularly, cytarabine is converted into cytarabine-5-triphosphate (ara-CTP), which is the active metabolite. The mechanism of action is not completely understood, but it appears that ara-CTP acts primarily through inhibition of DNA polymerase. Incorporation into DNA and RNA may also contribute to cytarabine cytotoxicity. Cytarabine is cytotoxic to a wide variety of proliferating mammalian cells in culture.The drug has a short plasma half-life, low stability and limited bioavailability. Overdosing of patients with continuous infusions may lead to side effects. Thus, various prodrug strategies and delivery systems have been explored extensively to enhance the half-life, stability and delivery of cytarabine. Alternative, delivery systems of cytarabine have emerged for the treatment of different cancers. The liposomal-cytarabine formulation has been approved for the treatment of lymphomatous meningitis.

CYTARABINE HYDROCHLORIDE

33K3DB6591

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Status:

US Approved Rx (1990)

First approved in 1969

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

DNA polymerase lambda

Conditions:

Chronic myelogenous leukemia

Lymphomatous meningitis

Cytarabine is a pyrimidine nucleoside analog. Cytarabine or cytosine arabinoside (Cytosar-U or Depocyt) is a chemotherapy agent used mainly in the treatment of cancers of white blood cells such as acute myeloid leukemia (AML) and non-Hodgkin lymphoma...

. It also has antiviral and immunosuppressant properties. Cytarabine is an antimetabolite antineoplastic agent that inhibits the synthesis of DNA. It is a cell cycle phase-specific, affecting cells only during the S phase of cell division. Intracellularly, cytarabine is converted into cytarabine-5-triphosphate (ara-CTP), which is the active metabolite. The mechanism of action is not completely understood, but it appears that ara-CTP acts primarily through inhibition of DNA polymerase. Incorporation into DNA and RNA may also contribute to cytarabine cytotoxicity. Cytarabine is cytotoxic to a wide variety of proliferating mammalian cells in culture.The drug has a short plasma half-life, low stability and limited bioavailability. Overdosing of patients with continuous infusions may lead to side effects. Thus, various prodrug strategies and delivery systems have been explored extensively to enhance the half-life, stability and delivery of cytarabine. Alternative, delivery systems of cytarabine have emerged for the treatment of different cancers. The liposomal-cytarabine formulation has been approved for the treatment of lymphomatous meningitis.

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