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Cytomegalovirus retinitis

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Unknown

2,596

Pain

619

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609

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575

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US Approved Rx

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Human herpesvirus 5 DNA polymerase

11

DNA polymerase catalytic subunit

8

Human herpesvirus 1 DNA polymerase

8

Human immunodeficiency virus type 1 reverse transcriptase

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1991

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1996

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Institute of Organic Chemistry and Biochemistry|Rega Institute for Medical Research

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AstraZeneca

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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 16 results

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CIDOFOVIR ANHYDROUS

768M1V522C

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Status:

US Approved Rx (2012)

First approved in 1996

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Human herpesvirus 1 DNA polymerase

Conditions:

Cytomegalovirus retinitis

Cidofovir is an antiviral nucleotide analogue with significant activity against cytomegalovirus (CMV) and other herpesviruses. Cidofovir suppresses cytomegalovirus (CMV) replication by selective inhibition of viral DNA synthesis. Biochemical data sup...

port selective inhibition of CMV DNA polymerase by cidofovir diphosphate, the active intracellular metabolite of cidofovir. Incorporation of cidofovir into the growing viral DNA chain results in reductions in the rate of viral DNA synthesis. Cidofovir is indicated for the treatment of CMV retinitis in patients with acquired immunodeficiency syndrome.

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.

CIDOFOVIR

JIL713Q00N

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Status:

US Approved Rx (2012)

First approved in 1996

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Human herpesvirus 1 DNA polymerase

Conditions:

Cytomegalovirus retinitis

Cidofovir is an antiviral nucleotide analogue with significant activity against cytomegalovirus (CMV) and other herpesviruses. Cidofovir suppresses cytomegalovirus (CMV) replication by selective inhibition of viral DNA synthesis. Biochemical data sup...

port selective inhibition of CMV DNA polymerase by cidofovir diphosphate, the active intracellular metabolite of cidofovir. Incorporation of cidofovir into the growing viral DNA chain results in reductions in the rate of viral DNA synthesis. Cidofovir is indicated for the treatment of CMV retinitis in patients with acquired immunodeficiency syndrome.

BRINCIDOFOVIR

6794O900AX

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Status:

US Approved Rx (2012)

First approved in 1996

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Human herpesvirus 1 DNA polymerase

Conditions:

Cytomegalovirus retinitis

Cidofovir is an antiviral nucleotide analogue with significant activity against cytomegalovirus (CMV) and other herpesviruses. Cidofovir suppresses cytomegalovirus (CMV) replication by selective inhibition of viral DNA synthesis. Biochemical data sup...

port selective inhibition of CMV DNA polymerase by cidofovir diphosphate, the active intracellular metabolite of cidofovir. Incorporation of cidofovir into the growing viral DNA chain results in reductions in the rate of viral DNA synthesis. Cidofovir is indicated for the treatment of CMV retinitis in patients with acquired immunodeficiency syndrome.

CIDOFOVIR SODIUM

M83JB37U61

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Status:

US Approved Rx (2012)

First approved in 1996

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Human herpesvirus 1 DNA polymerase

Conditions:

Cytomegalovirus retinitis

Cidofovir is an antiviral nucleotide analogue with significant activity against cytomegalovirus (CMV) and other herpesviruses. Cidofovir suppresses cytomegalovirus (CMV) replication by selective inhibition of viral DNA synthesis. Biochemical data sup...

port selective inhibition of CMV DNA polymerase by cidofovir diphosphate, the active intracellular metabolite of cidofovir. Incorporation of cidofovir into the growing viral DNA chain results in reductions in the rate of viral DNA synthesis. Cidofovir is indicated for the treatment of CMV retinitis in patients with acquired immunodeficiency syndrome.

BRINCIDOFOVIR SODIUM

8UN8SA9Z5C

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Status:

US Approved Rx (2012)

First approved in 1996

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Human herpesvirus 1 DNA polymerase

Conditions:

Cytomegalovirus retinitis

Cidofovir is an antiviral nucleotide analogue with significant activity against cytomegalovirus (CMV) and other herpesviruses. Cidofovir suppresses cytomegalovirus (CMV) replication by selective inhibition of viral DNA synthesis. Biochemical data sup...

port selective inhibition of CMV DNA polymerase by cidofovir diphosphate, the active intracellular metabolite of cidofovir. Incorporation of cidofovir into the growing viral DNA chain results in reductions in the rate of viral DNA synthesis. Cidofovir is indicated for the treatment of CMV retinitis in patients with acquired immunodeficiency syndrome.

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.

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