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Human herpesvirus 5 DNA polymerase

13

Histamine H1 receptor

316

Dopamine D2 receptor

311

DNA

282

Serotonin 2a (5-HT2a) receptor

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1989

8

1991

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Unknown

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Condition

Cytomegalovirus retinitis

11

Acute herpetic keratitis

8

Cytomegalovirus infectious disease in kidney, heart, and kidney-pancreas transplantation

8

Unknown

8

Cancer

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CNS Penetrant

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AstraZeneca

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FDA UNII

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PUBCHEM

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EPA CompTox

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EVMPD

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ANTIINFECTIVES FOR SYSTEMIC USE

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DIRECT ACTING ANTIVIRALS

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Nucleosides and nucleotides excl. reverse transcriptase inhibitors

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Antivirals

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Phosphonic acid derivatives

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Showing 1 - 10 of 13 results

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FOSCARNET

364P9RVW4X

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Status:

US Approved Rx (2024)

First approved in 1991

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Human herpesvirus 5 DNA polymerase

Human immunodeficiency virus type 1 reverse transcriptase

Human herpesvirus 1 DNA polymerase

Conditions:

Cytomegalovirus retinitis

Foscarnet is an antiviral agent. Foscarnet shows activity against human herpesviruses and HIV. Foscarnet is used for treating eye problems caused by CMV in people with AIDS. It is also used to treat a type of HSV that cannot be treated by another med...

icine in people with a weak immune system. FOSCAVIR is the brand name for foscarnet sodium. FOSCAVIR is an organic analogue of inorganic pyrophosphate that inhibits replication of herpesviruses in vitro including cytomegalovirus (CMV) and herpes simplex virus types 1 and 2 (HSV-1 and HSV-2). FOSCAVIR exerts its antiviral activity by a selective inhibition at the pyrophosphate binding site on virusspecific DNA polymerases at concentrations that do not affect cellular DNA polymerases. FOSCAVIR does not require activation (phosphorylation) by thymidine kinase or other kinases and therefore is active in vitro against HSV TK deficient mutants and CMV UL97 mutants. Thus, HSV strains resistant to acyclovir or CMV strains resistant to ganciclovir may be sensitive to FOSCAVIR.

Ganciclovir

P9G3CKZ4P5

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Status:

US Approved Rx (2016)

First approved in 1989

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Human herpesvirus 5 DNA polymerase

DNA polymerase catalytic subunit

Conditions:

Cytomegalovirus retinitis

Cytomegalovirus infectious disease in kidney, heart, and kidney-pancreas transplantation

Cytomegalovirus retinitis

Acute herpetic keratitis

Ganciclovir is a synthetic acyclic nucleoside analogue of 2'-deoxyguanosine active against cytomegalovirus. Ganciclovir has been shown to be active against cytomegalovirus (CMV) and herpes simplex virus (HSV) in humans. To achieve anti-CMV activity, ...

ganciclovir is phosphorylated first to the monophosphate form by a CMV-encoded (UL97 gene) protein kinase homologue, then to the di- and triphosphate forms by cellular kinases. Ganciclovir triphosphate concentrations may be 100-fold greater in CMV-infected than in uninfected cells, indicating preferential phosphorylation in infected cells. Ganciclovir triphosphate, once formed, persists for days in the CMV-infected cell. Ganciclovir triphosphate is believed to inhibit viral DNA synthesis by (1) competitive inhibition of viral DNA polymerases; and (2) incorporation into viral DNA, resulting in eventual termination of viral DNA elongation. Ganciclovir is indicated for the treatment of CMV retinitis in immunocompromised patients, including patients with acquired immunodeficiency syndrome (AIDS) and for the treatment of acute herpetic keratitis.

APHIDICOLIN, (±)-

6B3F8QW8TU

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Status:

Designated

Class (Stereo):

CHEMICAL (RACEMIC)

Targets:

Human herpesvirus 5 DNA polymerase

Human herpesvirus 1

DNA polymerase alpha subunit

Conditions:

Herpes virus infections

Aphidicolin, a tetracyclic diterpenoid obtained from the culture filtrates of Cephalosporium aphidicola and other fungi, inhibits the growth of eukaryotic cells and of certain animal viruses (SV40, Herpes and Vaccinia viruses) by selectively inhibiti...

ng the cellular replicative DNA polymerase alpha or the viral-induced DNA polymerases. The arrest of cellular or viral growth is thus due to inhibition of cellular or viral replicative DNA synthesis without interference with mitochondrial DNA synthesis, RNA, protein and nucleic acid precursors synthesis or other major metabolic pathways. The inhibition of all sensitive eukaryotic DNA polymerases by aphidicolin is competitive with respect to dCTP. Aphidicolin has thus proved extremely useful in elucidating the functional role of DNA polymerase alpha in nuclear DNA replication, of DNA polymerase gamma in mitochondrial DNA synthesis and both DNA polymerases beta and alpha in DNA repair synthesis. An important laboratory application of aphidicolin is the synchronization of the cell cycle of eukaryotic cells both in culture and in vivo. The properties of aphidicolinhave recently aroused considerable interest for its possible exploitation in al practice. The mechanism of action of this drug suggests in fact that it may be useful for controlling excessive cell proliferation in patients with cancer, psoriasis or other dermatitis with little or no adverse effect upon non-multiplying cells.

FOSCARNET SODIUM ANHYDROUS

8C5OQ81LWT

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Status:

US Approved Rx (2024)

First approved in 1991

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Human herpesvirus 5 DNA polymerase

Human immunodeficiency virus type 1 reverse transcriptase

Human herpesvirus 1 DNA polymerase

Conditions:

Cytomegalovirus retinitis

Foscarnet is an antiviral agent. Foscarnet shows activity against human herpesviruses and HIV. Foscarnet is used for treating eye problems caused by CMV in people with AIDS. It is also used to treat a type of HSV that cannot be treated by another med...

icine in people with a weak immune system. FOSCAVIR is the brand name for foscarnet sodium. FOSCAVIR is an organic analogue of inorganic pyrophosphate that inhibits replication of herpesviruses in vitro including cytomegalovirus (CMV) and herpes simplex virus types 1 and 2 (HSV-1 and HSV-2). FOSCAVIR exerts its antiviral activity by a selective inhibition at the pyrophosphate binding site on virusspecific DNA polymerases at concentrations that do not affect cellular DNA polymerases. FOSCAVIR does not require activation (phosphorylation) by thymidine kinase or other kinases and therefore is active in vitro against HSV TK deficient mutants and CMV UL97 mutants. Thus, HSV strains resistant to acyclovir or CMV strains resistant to ganciclovir may be sensitive to FOSCAVIR.

Foscarnet Sodium

964YS0OOG1

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Status:

US Approved Rx (2024)

First approved in 1991

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Human herpesvirus 5 DNA polymerase

Human immunodeficiency virus type 1 reverse transcriptase

Human herpesvirus 1 DNA polymerase

Conditions:

Cytomegalovirus retinitis

Foscarnet is an antiviral agent. Foscarnet shows activity against human herpesviruses and HIV. Foscarnet is used for treating eye problems caused by CMV in people with AIDS. It is also used to treat a type of HSV that cannot be treated by another med...

icine in people with a weak immune system. FOSCAVIR is the brand name for foscarnet sodium. FOSCAVIR is an organic analogue of inorganic pyrophosphate that inhibits replication of herpesviruses in vitro including cytomegalovirus (CMV) and herpes simplex virus types 1 and 2 (HSV-1 and HSV-2). FOSCAVIR exerts its antiviral activity by a selective inhibition at the pyrophosphate binding site on virusspecific DNA polymerases at concentrations that do not affect cellular DNA polymerases. FOSCAVIR does not require activation (phosphorylation) by thymidine kinase or other kinases and therefore is active in vitro against HSV TK deficient mutants and CMV UL97 mutants. Thus, HSV strains resistant to acyclovir or CMV strains resistant to ganciclovir may be sensitive to FOSCAVIR.

Valganciclovir Hydrochloride

4P3T9QF9NZ

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Status:

US Approved Rx (2016)

First approved in 1989

Class (Stereo):

CHEMICAL (EPIMERIC)

Targets:

Human herpesvirus 5 DNA polymerase

DNA polymerase catalytic subunit

Conditions:

Cytomegalovirus retinitis

Cytomegalovirus infectious disease in kidney, heart, and kidney-pancreas transplantation

Cytomegalovirus retinitis

Acute herpetic keratitis

Ganciclovir is a synthetic acyclic nucleoside analogue of 2'-deoxyguanosine active against cytomegalovirus. Ganciclovir has been shown to be active against cytomegalovirus (CMV) and herpes simplex virus (HSV) in humans. To achieve anti-CMV activity, ...

ganciclovir is phosphorylated first to the monophosphate form by a CMV-encoded (UL97 gene) protein kinase homologue, then to the di- and triphosphate forms by cellular kinases. Ganciclovir triphosphate concentrations may be 100-fold greater in CMV-infected than in uninfected cells, indicating preferential phosphorylation in infected cells. Ganciclovir triphosphate, once formed, persists for days in the CMV-infected cell. Ganciclovir triphosphate is believed to inhibit viral DNA synthesis by (1) competitive inhibition of viral DNA polymerases; and (2) incorporation into viral DNA, resulting in eventual termination of viral DNA elongation. Ganciclovir is indicated for the treatment of CMV retinitis in immunocompromised patients, including patients with acquired immunodeficiency syndrome (AIDS) and for the treatment of acute herpetic keratitis.

VALGANCICLOVIR

GCU97FKN3R

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Status:

US Approved Rx (2016)

First approved in 1989

Class (Stereo):

CHEMICAL (EPIMERIC)

Targets:

Human herpesvirus 5 DNA polymerase

DNA polymerase catalytic subunit

Conditions:

Cytomegalovirus retinitis

Cytomegalovirus infectious disease in kidney, heart, and kidney-pancreas transplantation

Cytomegalovirus retinitis

Acute herpetic keratitis

Ganciclovir is a synthetic acyclic nucleoside analogue of 2'-deoxyguanosine active against cytomegalovirus. Ganciclovir has been shown to be active against cytomegalovirus (CMV) and herpes simplex virus (HSV) in humans. To achieve anti-CMV activity, ...

ganciclovir is phosphorylated first to the monophosphate form by a CMV-encoded (UL97 gene) protein kinase homologue, then to the di- and triphosphate forms by cellular kinases. Ganciclovir triphosphate concentrations may be 100-fold greater in CMV-infected than in uninfected cells, indicating preferential phosphorylation in infected cells. Ganciclovir triphosphate, once formed, persists for days in the CMV-infected cell. Ganciclovir triphosphate is believed to inhibit viral DNA synthesis by (1) competitive inhibition of viral DNA polymerases; and (2) incorporation into viral DNA, resulting in eventual termination of viral DNA elongation. Ganciclovir is indicated for the treatment of CMV retinitis in immunocompromised patients, including patients with acquired immunodeficiency syndrome (AIDS) and for the treatment of acute herpetic keratitis.

ROCICLOVIR

6DF29U51Y7

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Status:

US Approved Rx (2016)

First approved in 1989

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Human herpesvirus 5 DNA polymerase

DNA polymerase catalytic subunit

Conditions:

Cytomegalovirus retinitis

Cytomegalovirus infectious disease in kidney, heart, and kidney-pancreas transplantation

Cytomegalovirus retinitis

Acute herpetic keratitis

Ganciclovir is a synthetic acyclic nucleoside analogue of 2'-deoxyguanosine active against cytomegalovirus. Ganciclovir has been shown to be active against cytomegalovirus (CMV) and herpes simplex virus (HSV) in humans. To achieve anti-CMV activity, ...

ganciclovir is phosphorylated first to the monophosphate form by a CMV-encoded (UL97 gene) protein kinase homologue, then to the di- and triphosphate forms by cellular kinases. Ganciclovir triphosphate concentrations may be 100-fold greater in CMV-infected than in uninfected cells, indicating preferential phosphorylation in infected cells. Ganciclovir triphosphate, once formed, persists for days in the CMV-infected cell. Ganciclovir triphosphate is believed to inhibit viral DNA synthesis by (1) competitive inhibition of viral DNA polymerases; and (2) incorporation into viral DNA, resulting in eventual termination of viral DNA elongation. Ganciclovir is indicated for the treatment of CMV retinitis in immunocompromised patients, including patients with acquired immunodeficiency syndrome (AIDS) and for the treatment of acute herpetic keratitis.

VALINE-VALINE-GANCICLOVIR

ZW811N4EW6

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Status:

US Approved Rx (2016)

First approved in 1989

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Human herpesvirus 5 DNA polymerase

DNA polymerase catalytic subunit

Conditions:

Cytomegalovirus retinitis

Cytomegalovirus infectious disease in kidney, heart, and kidney-pancreas transplantation

Cytomegalovirus retinitis

Acute herpetic keratitis

Ganciclovir is a synthetic acyclic nucleoside analogue of 2'-deoxyguanosine active against cytomegalovirus. Ganciclovir has been shown to be active against cytomegalovirus (CMV) and herpes simplex virus (HSV) in humans. To achieve anti-CMV activity, ...

ganciclovir is phosphorylated first to the monophosphate form by a CMV-encoded (UL97 gene) protein kinase homologue, then to the di- and triphosphate forms by cellular kinases. Ganciclovir triphosphate concentrations may be 100-fold greater in CMV-infected than in uninfected cells, indicating preferential phosphorylation in infected cells. Ganciclovir triphosphate, once formed, persists for days in the CMV-infected cell. Ganciclovir triphosphate is believed to inhibit viral DNA synthesis by (1) competitive inhibition of viral DNA polymerases; and (2) incorporation into viral DNA, resulting in eventual termination of viral DNA elongation. Ganciclovir is indicated for the treatment of CMV retinitis in immunocompromised patients, including patients with acquired immunodeficiency syndrome (AIDS) and for the treatment of acute herpetic keratitis.

Valganciclovir Hydrochloride, (R)-

FR5B7CU4CF

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Status:

US Approved Rx (2016)

First approved in 1989

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Human herpesvirus 5 DNA polymerase

DNA polymerase catalytic subunit

Conditions:

Cytomegalovirus retinitis

Cytomegalovirus infectious disease in kidney, heart, and kidney-pancreas transplantation

Cytomegalovirus retinitis

Acute herpetic keratitis

Ganciclovir is a synthetic acyclic nucleoside analogue of 2'-deoxyguanosine active against cytomegalovirus. Ganciclovir has been shown to be active against cytomegalovirus (CMV) and herpes simplex virus (HSV) in humans. To achieve anti-CMV activity, ...

ganciclovir is phosphorylated first to the monophosphate form by a CMV-encoded (UL97 gene) protein kinase homologue, then to the di- and triphosphate forms by cellular kinases. Ganciclovir triphosphate concentrations may be 100-fold greater in CMV-infected than in uninfected cells, indicating preferential phosphorylation in infected cells. Ganciclovir triphosphate, once formed, persists for days in the CMV-infected cell. Ganciclovir triphosphate is believed to inhibit viral DNA synthesis by (1) competitive inhibition of viral DNA polymerases; and (2) incorporation into viral DNA, resulting in eventual termination of viral DNA elongation. Ganciclovir is indicated for the treatment of CMV retinitis in immunocompromised patients, including patients with acquired immunodeficiency syndrome (AIDS) and for the treatment of acute herpetic keratitis.

Showing 1 - 10 of 13 results

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