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US Approved Rx

9

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Primary Target

DNA

6

DNA polymerase lambda

3

CAKI-1

2

MIA PaCa-2

2

PANC-1

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Highest Phase

Approved

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Approval Year

1964

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1969

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1996

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Condition

Epithelial carcinoma of the ovary

4

Multiple myeloma

4

Relapsed or refractory multiple myeloma

4

Chronic myelogenous leukemia

3

Lymphomatous meningitis

3

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Treatment Modality

Primary

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Palliative

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CNS Activity

CNS Penetrant

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CNS Active

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Originator

Chester Beatty Research Institute|Larionov, L.F.|Blokhin, N.

4

University of California-Berkeley

3

Eli Lilly|University of Innsbruck

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CAS

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FDA UNII

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PUBCHEM

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EPA CompTox

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NCI_THESAURUS

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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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ALKYLATING AGENTS

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OTHER ANTINEOPLASTIC AGENTS

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ATC Level 4

Pyrimidine analogues

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Nitrogen mustard analogues

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Showing 1 - 9 of 9 results

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GEMCITABINE HYDROCHLORIDE

U347PV74IL

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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.

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.

MELPHALAN

Q41OR9510P

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Status:

US Approved Rx (2023)

First approved in 1964

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Conditions:

Relapsed or refractory multiple myeloma

Epithelial carcinoma of the ovary

Multiple myeloma

Melphalan, also known as L-phenylalanine mustard, phenylalanine mustard, L-PAM, or L-sarcolysin, is a phenylalanine derivative of nitrogen mustard. Melphalan is a bifunctional alkylating agent which produces a number of DNA adducts with the DNA inter...

strand crosslink (ICL) considered to be the critical cytotoxic lesion. Melphalan is used to treat different cancers including myeloma, melanoma and ovarian cancer.

GEMCITABINE

B76N6SBZ8R

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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.

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.

MELPHALAN FLUFENAMIDE HYDROCHLORIDE

3412470A0V

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Status:

US Approved Rx (2023)

First approved in 1964

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Conditions:

Relapsed or refractory multiple myeloma

Epithelial carcinoma of the ovary

Multiple myeloma

Melphalan, also known as L-phenylalanine mustard, phenylalanine mustard, L-PAM, or L-sarcolysin, is a phenylalanine derivative of nitrogen mustard. Melphalan is a bifunctional alkylating agent which produces a number of DNA adducts with the DNA inter...

strand crosslink (ICL) considered to be the critical cytotoxic lesion. Melphalan is used to treat different cancers including myeloma, melanoma and ovarian cancer.

MELPHALAN FLUFENAMIDE

F70C5K4786

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Status:

US Approved Rx (2023)

First approved in 1964

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Conditions:

Relapsed or refractory multiple myeloma

Epithelial carcinoma of the ovary

Multiple myeloma

Melphalan, also known as L-phenylalanine mustard, phenylalanine mustard, L-PAM, or L-sarcolysin, is a phenylalanine derivative of nitrogen mustard. Melphalan is a bifunctional alkylating agent which produces a number of DNA adducts with the DNA inter...

strand crosslink (ICL) considered to be the critical cytotoxic lesion. Melphalan is used to treat different cancers including myeloma, melanoma and ovarian cancer.

Melphalan hydrochloride

1VXP4V453T

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Status:

US Approved Rx (2023)

First approved in 1964

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Conditions:

Relapsed or refractory multiple myeloma

Epithelial carcinoma of the ovary

Multiple myeloma

Melphalan, also known as L-phenylalanine mustard, phenylalanine mustard, L-PAM, or L-sarcolysin, is a phenylalanine derivative of nitrogen mustard. Melphalan is a bifunctional alkylating agent which produces a number of DNA adducts with the DNA inter...

strand crosslink (ICL) considered to be the critical cytotoxic lesion. Melphalan is used to treat different cancers including myeloma, melanoma and ovarian cancer.

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