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US Approved Rx

8

US Previously Marketed

2

Possibly Marketed Outside US

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Primary Target

DNA polymerase catalytic subunit

8

Human herpesvirus 5 DNA polymerase

8

AMP-activated protein kinase, AMPK

2

Mammalian target of Rapamycin (mTORC1)

2

Monoamine oxidase A

2

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Highest Phase

Approved

11

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Approval Year

1989

8

1959

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Unknown

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Condition

Acute herpetic keratitis

8

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

8

Cytomegalovirus retinitis

8

Unknown

8

Breast cancer

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Treatment Modality

Primary

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CNS Activity

CNS Penetrant

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CNS Active

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Syntex

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US Vitamin Pharm

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Daiichi Sankyo|Ube Industries

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Chemical

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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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ChEMBL

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ATC Level 1

ANTIINFECTIVES FOR SYSTEMIC USE

2

ALIMENTARY TRACT AND METABOLISM

1

SENSORY ORGANS

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ATC Level 2

ANTIVIRALS FOR SYSTEMIC USE

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DRUGS USED IN DIABETES

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OPHTHALMOLOGICALS

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ATC Level 3

DIRECT ACTING ANTIVIRALS

2

ANTIINFECTIVES

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BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS

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ATC Level 4

Nucleosides and nucleotides excl. reverse transcriptase inhibitors

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Antivirals

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Biguanides

1

Combinations of oral blood glucose lowering drugs

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Salts, Hydrates, Esters, etc.

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Principal Form

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Showing 1 - 10 of 11 results

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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.

PHENFORMIN

DD5K7529CE

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Status:

US Previously Marketed

First approved in 1959

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Sulfonylurea receptors; K-ATP channels

Mammalian target of Rapamycin (mTORC1)

AMP-activated protein kinase, AMPK

Monoamine oxidase A

Conditions:

Type 2 diabetes mellitus

Phenformin is a biguanide hypoglycemic agent with actions and uses similar to those of metformin. It activates AMP-activated protein kinase (AMPK) and inhibits mTORC1 signaling. Phenformin used for the treatment of diabetes. Phenformin was removed fr...

om the U.S. market 20 years ago because of a high incidence of lactic acidosis. Risk factors for the development of lactic acidosis include renal deficiency, hepatic disease, cardiac disease, and drug interaction such as cimetidine. Phenformin exerts potential anti-neoplastic action.

AZELNIDIPINE

PV23P19YUG

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Status:

Possibly Marketed Outside US

Class (Stereo):

CHEMICAL (RACEMIC)

Targets:

Voltage-gated L-type calcium channel

Voltage-gated T-type calcium channel

Conditions:

Azelnidipine (INN; marketed under the brand name CalBlock) is a dihydropyridine calcium channel blocker. It is sold in Japan by Daiichi-Sankyo pharmaceuticals, Inc. Azelnidipine is a new dihydropyridine calcium channel antagonist with selectivity for...

both L-type and T-type Ca channels. It has recently been approved in Japan for the treatment of patients with hypertension. Results from clinical trials showed that long-term treatment with azelnidipine effectively controls blood pressure (BP) in a cohort of 95 patients with mild-to-moderate hypertension. The antihypertensive efficacy of azelnidipine in patients with mild-to-moderate hypertension was shown to be similar to that of amlodipine or nitrendipine in a randomised double-blind study. Azelnidipine and amlodipine controlled 24-hour BP to a similar extent. Azelnidipine is generally well tolerated. Vasodilator adverse events such as headache and hot facial flushes account for most of the adverse events. Its use is not associated with reflex tachycardia.

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.

VALGANCICLOVIR, (R)-

H61CHR8D70

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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.

GANCICLOVIR SODIUM

02L083W284

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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.

Showing 1 - 10 of 11 results

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