Inxight Drugs

U.S. Department of Health & Human Services Divider Arrow

National Institutes of Health Divider Arrow

NCATS

Return Home Inxight Drugs

Home
Browse Drugs
Search
- Structure Search
- Sequence Search
Downloads
About

Show Filters

Hide Filters

Development Status

US Approved Rx

11

All Match

Any Match

Exclude Selected

Exclude Selected

Primary Target

Human herpesvirus 1 DNA polymerase

8

Thymidine kinase

8

DNA topoisomerase II

3

All Match

Any Match

Exclude Selected

Exclude Selected

Highest Phase

Approved

11

All Match

Any Match

Exclude Selected

Exclude Selected

Approval Year

1982

8

1983

3

All Match

Any Match

Exclude Selected

Exclude Selected

Condition

Cold sores

8

Genital herpes

8

Herpes simplex infection

8

Herpes zoster infections

8

Refractory testicular tumors

3

All Match

Any Match

Exclude Selected

Exclude Selected

Treatment Modality

Primary

11

All Match

Any Match

Exclude Selected

Exclude Selected

CNS Activity

CNS Penetrant

8

CNS Active

3

All Match

Any Match

Exclude Selected

Exclude Selected

Originator

Burroughs Wellcome Fund

8

All Match

Any Match

Exclude Selected

Exclude Selected

Substance Class

Chemical

11

All Match

Any Match

Exclude Selected

Exclude Selected

Code System

CAS

11

FDA UNII

11

PUBCHEM

11

SMS_ID

10

EPA CompTox

8

All Match

Any Match

Exclude Selected

Exclude Selected

ATC Level 1

ANTIINFECTIVES FOR SYSTEMIC USE

2

ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

1

DERMATOLOGICALS

1

SENSORY ORGANS

1

All Match

Any Match

Exclude Selected

Exclude Selected

ATC Level 2

ANTIVIRALS FOR SYSTEMIC USE

2

ANTIBIOTICS AND CHEMOTHERAPEUTICS FOR DERMATOLOGICAL USE

1

ANTINEOPLASTIC AGENTS

1

OPHTHALMOLOGICALS

1

All Match

Any Match

Exclude Selected

Exclude Selected

ATC Level 3

DIRECT ACTING ANTIVIRALS

2

ANTIINFECTIVES

1

CHEMOTHERAPEUTICS FOR TOPICAL USE

1

PLANT ALKALOIDS AND OTHER NATURAL PRODUCTS

1

All Match

Any Match

Exclude Selected

Exclude Selected

ATC Level 4

Nucleosides and nucleotides excl. reverse transcriptase inhibitors

2

Antivirals

1

Podophyllotoxin derivatives

1

All Match

Any Match

Exclude Selected

Exclude Selected

Substance Form

Salts, Hydrates, Esters, etc.

9

Principal Form

2

All Match

Any Match

Exclude Selected

Exclude Selected

Showing 1 - 10 of 11 results

First page disabled
Previous page disabled
1
Next page
Next page

ETOPOSIDE

6PLQ3CP4P3

Export Data
Search for Structure

Status:

US Approved Rx (1998)

First approved in 1983

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

DNA topoisomerase II

Conditions:

Refractory testicular tumors

Small-cell lung cancer

Etoposide (trade name Etopophos) is a semisynthetic derivative of podophyllotoxin that exhibits antitumor activity. It has been in clinical use for more than two decades and remains one of the most highly prescribed anticancer drugs in the world. The...

primary cytotoxic target for etoposide is topoisomerase II. This ubiquitous enzyme regulates DNA under- and over winding, and removes knots and tangles from the genome by generating transient double-stranded breaks in the double helix. Etoposide kills cells by stabilizing a covalent enzyme-cleaved DNA complex (known as the cleavage complex) that is a transient intermediate in the catalytic cycle of topoisomerase II. The accumulation of cleavage complexes in treated cells leads to the generation of permanent DNA strand breaks, which trigger recombination/repair pathways, mutagenesis, and chromosomal translocations. If these breaks overwhelm the cell, they can initiate death pathways. Thus, etoposide converts topoisomerase II from an essential enzyme to a potent cellular toxin that fragments the genome. Although the topoisomerase II-DNA cleavage complex is an important target for cancer chemotherapy, there also is evidence that topoisomerase II-mediated DNA strand breaks induced by etoposide and other agents can trigger chromosomal translocations that lead to specific types of leukemia. Etopophos (etoposide phosphate) is indicated in the management of the following neoplasms: Refractory Testicular Tumors-and for Small Cell Lung Cancer. The in vitro cytotoxicity observed for etoposide phosphate is significantly less than that seen with etoposide, which is believed due to the necessity for conversion in vivo to the active moiety, etoposide, by dephosphorylation. The mechanism of action is believed to be the same as that of etoposide.

ACYCLOVIR

X4HES1O11F

Export Data
Search for Structure

Status:

US Approved Rx (2019)

First approved in 1982

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Thymidine kinase

Human herpesvirus 1 DNA polymerase

Conditions:

Herpes zoster infections

Herpes simplex infection

Herpes zoster infections

Acyclovir is a synthetic antiviral nucleoside analogue. A screening program for antiviral drugs begun at Burroughs Wellcome in the 1960s resulted in the discovery of acyclovir in 1974. Preclinical investigation brought the drug to clinical trials in ...

1977 and the first form of the drug (topical) was available to physicians in 1982. Activity of acyclovir is greatest against herpes 1 and herpes 2, less against varicella zoster, still less against Epstein-Barr, and very little against cytomegalovirus. Acyclovir is an antiviral agent only after it is phosphorylated in infected cells by a viral-induced thymidine kinase. Acyclovir monophosphate is phosphorylated to diphosphate and triphosphate forms by cellular enzymes in the infected host cell where the drug is concentrated. Acyclovir triphosphate inactivates viral deoxyribonucleic acid polymerase.

ETOPOSIDE TONIRIBATE

A59HL2Q48U

Export Data
Search for Structure

Status:

US Approved Rx (1998)

First approved in 1983

Class (Stereo):

CHEMICAL (EPIMERIC)

Targets:

DNA topoisomerase II

Conditions:

Refractory testicular tumors

Small-cell lung cancer

Etoposide (trade name Etopophos) is a semisynthetic derivative of podophyllotoxin that exhibits antitumor activity. It has been in clinical use for more than two decades and remains one of the most highly prescribed anticancer drugs in the world. The...

primary cytotoxic target for etoposide is topoisomerase II. This ubiquitous enzyme regulates DNA under- and over winding, and removes knots and tangles from the genome by generating transient double-stranded breaks in the double helix. Etoposide kills cells by stabilizing a covalent enzyme-cleaved DNA complex (known as the cleavage complex) that is a transient intermediate in the catalytic cycle of topoisomerase II. The accumulation of cleavage complexes in treated cells leads to the generation of permanent DNA strand breaks, which trigger recombination/repair pathways, mutagenesis, and chromosomal translocations. If these breaks overwhelm the cell, they can initiate death pathways. Thus, etoposide converts topoisomerase II from an essential enzyme to a potent cellular toxin that fragments the genome. Although the topoisomerase II-DNA cleavage complex is an important target for cancer chemotherapy, there also is evidence that topoisomerase II-mediated DNA strand breaks induced by etoposide and other agents can trigger chromosomal translocations that lead to specific types of leukemia. Etopophos (etoposide phosphate) is indicated in the management of the following neoplasms: Refractory Testicular Tumors-and for Small Cell Lung Cancer. The in vitro cytotoxicity observed for etoposide phosphate is significantly less than that seen with etoposide, which is believed due to the necessity for conversion in vivo to the active moiety, etoposide, by dephosphorylation. The mechanism of action is believed to be the same as that of etoposide.

ETOPOSIDE PHOSPHATE

528XYJ8L1N

Export Data
Search for Structure

Status:

US Approved Rx (1998)

First approved in 1983

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

DNA topoisomerase II

Conditions:

Refractory testicular tumors

Small-cell lung cancer

Etoposide (trade name Etopophos) is a semisynthetic derivative of podophyllotoxin that exhibits antitumor activity. It has been in clinical use for more than two decades and remains one of the most highly prescribed anticancer drugs in the world. The...

primary cytotoxic target for etoposide is topoisomerase II. This ubiquitous enzyme regulates DNA under- and over winding, and removes knots and tangles from the genome by generating transient double-stranded breaks in the double helix. Etoposide kills cells by stabilizing a covalent enzyme-cleaved DNA complex (known as the cleavage complex) that is a transient intermediate in the catalytic cycle of topoisomerase II. The accumulation of cleavage complexes in treated cells leads to the generation of permanent DNA strand breaks, which trigger recombination/repair pathways, mutagenesis, and chromosomal translocations. If these breaks overwhelm the cell, they can initiate death pathways. Thus, etoposide converts topoisomerase II from an essential enzyme to a potent cellular toxin that fragments the genome. Although the topoisomerase II-DNA cleavage complex is an important target for cancer chemotherapy, there also is evidence that topoisomerase II-mediated DNA strand breaks induced by etoposide and other agents can trigger chromosomal translocations that lead to specific types of leukemia. Etopophos (etoposide phosphate) is indicated in the management of the following neoplasms: Refractory Testicular Tumors-and for Small Cell Lung Cancer. The in vitro cytotoxicity observed for etoposide phosphate is significantly less than that seen with etoposide, which is believed due to the necessity for conversion in vivo to the active moiety, etoposide, by dephosphorylation. The mechanism of action is believed to be the same as that of etoposide.

Acyclovir Sodium Dihydrate

TZT3J8XU9F

Export Data
Search for Structure

Status:

US Approved Rx (2019)

First approved in 1982

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Thymidine kinase

Human herpesvirus 1 DNA polymerase

Conditions:

Herpes zoster infections

Herpes simplex infection

Herpes zoster infections

Acyclovir is a synthetic antiviral nucleoside analogue. A screening program for antiviral drugs begun at Burroughs Wellcome in the 1960s resulted in the discovery of acyclovir in 1974. Preclinical investigation brought the drug to clinical trials in ...

1977 and the first form of the drug (topical) was available to physicians in 1982. Activity of acyclovir is greatest against herpes 1 and herpes 2, less against varicella zoster, still less against Epstein-Barr, and very little against cytomegalovirus. Acyclovir is an antiviral agent only after it is phosphorylated in infected cells by a viral-induced thymidine kinase. Acyclovir monophosphate is phosphorylated to diphosphate and triphosphate forms by cellular enzymes in the infected host cell where the drug is concentrated. Acyclovir triphosphate inactivates viral deoxyribonucleic acid polymerase.

VALACYCLOVIR

MZ1IW7Q79D

Export Data
Search for Structure

Status:

US Approved Rx (2019)

First approved in 1982

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Thymidine kinase

Human herpesvirus 1 DNA polymerase

Conditions:

Herpes zoster infections

Herpes simplex infection

Herpes zoster infections

Acyclovir is a synthetic antiviral nucleoside analogue. A screening program for antiviral drugs begun at Burroughs Wellcome in the 1960s resulted in the discovery of acyclovir in 1974. Preclinical investigation brought the drug to clinical trials in ...

1977 and the first form of the drug (topical) was available to physicians in 1982. Activity of acyclovir is greatest against herpes 1 and herpes 2, less against varicella zoster, still less against Epstein-Barr, and very little against cytomegalovirus. Acyclovir is an antiviral agent only after it is phosphorylated in infected cells by a viral-induced thymidine kinase. Acyclovir monophosphate is phosphorylated to diphosphate and triphosphate forms by cellular enzymes in the infected host cell where the drug is concentrated. Acyclovir triphosphate inactivates viral deoxyribonucleic acid polymerase.

VALACYCLOVIR HYDROCHLORIDE MONOHYDRATE

JF64RVR4E3

Export Data
Search for Structure

Status:

US Approved Rx (2019)

First approved in 1982

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Thymidine kinase

Human herpesvirus 1 DNA polymerase

Conditions:

Herpes zoster infections

Herpes simplex infection

Herpes zoster infections

Acyclovir is a synthetic antiviral nucleoside analogue. A screening program for antiviral drugs begun at Burroughs Wellcome in the 1960s resulted in the discovery of acyclovir in 1974. Preclinical investigation brought the drug to clinical trials in ...

1977 and the first form of the drug (topical) was available to physicians in 1982. Activity of acyclovir is greatest against herpes 1 and herpes 2, less against varicella zoster, still less against Epstein-Barr, and very little against cytomegalovirus. Acyclovir is an antiviral agent only after it is phosphorylated in infected cells by a viral-induced thymidine kinase. Acyclovir monophosphate is phosphorylated to diphosphate and triphosphate forms by cellular enzymes in the infected host cell where the drug is concentrated. Acyclovir triphosphate inactivates viral deoxyribonucleic acid polymerase.

ACYCLOVIR SODIUM

927L42J563

Export Data
Search for Structure

Status:

US Approved Rx (2019)

First approved in 1982

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Thymidine kinase

Human herpesvirus 1 DNA polymerase

Conditions:

Herpes zoster infections

Herpes simplex infection

Herpes zoster infections

Acyclovir is a synthetic antiviral nucleoside analogue. A screening program for antiviral drugs begun at Burroughs Wellcome in the 1960s resulted in the discovery of acyclovir in 1974. Preclinical investigation brought the drug to clinical trials in ...

1977 and the first form of the drug (topical) was available to physicians in 1982. Activity of acyclovir is greatest against herpes 1 and herpes 2, less against varicella zoster, still less against Epstein-Barr, and very little against cytomegalovirus. Acyclovir is an antiviral agent only after it is phosphorylated in infected cells by a viral-induced thymidine kinase. Acyclovir monophosphate is phosphorylated to diphosphate and triphosphate forms by cellular enzymes in the infected host cell where the drug is concentrated. Acyclovir triphosphate inactivates viral deoxyribonucleic acid polymerase.

VALACYCLOVIR HYDROCHLORIDE DIHYDRATE

A7JO128919

Export Data
Search for Structure

Status:

US Approved Rx (2019)

First approved in 1982

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Thymidine kinase

Human herpesvirus 1 DNA polymerase

Conditions:

Herpes zoster infections

Herpes simplex infection

Herpes zoster infections

Acyclovir is a synthetic antiviral nucleoside analogue. A screening program for antiviral drugs begun at Burroughs Wellcome in the 1960s resulted in the discovery of acyclovir in 1974. Preclinical investigation brought the drug to clinical trials in ...

1977 and the first form of the drug (topical) was available to physicians in 1982. Activity of acyclovir is greatest against herpes 1 and herpes 2, less against varicella zoster, still less against Epstein-Barr, and very little against cytomegalovirus. Acyclovir is an antiviral agent only after it is phosphorylated in infected cells by a viral-induced thymidine kinase. Acyclovir monophosphate is phosphorylated to diphosphate and triphosphate forms by cellular enzymes in the infected host cell where the drug is concentrated. Acyclovir triphosphate inactivates viral deoxyribonucleic acid polymerase.

VALACYCLOVIR HYDROCHLORIDE

G447S0T1VC

Export Data
Search for Structure

Status:

US Approved Rx (2019)

First approved in 1982

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Thymidine kinase

Human herpesvirus 1 DNA polymerase

Conditions:

Herpes zoster infections

Herpes simplex infection

Herpes zoster infections

Acyclovir is a synthetic antiviral nucleoside analogue. A screening program for antiviral drugs begun at Burroughs Wellcome in the 1960s resulted in the discovery of acyclovir in 1974. Preclinical investigation brought the drug to clinical trials in ...

1977 and the first form of the drug (topical) was available to physicians in 1982. Activity of acyclovir is greatest against herpes 1 and herpes 2, less against varicella zoster, still less against Epstein-Barr, and very little against cytomegalovirus. Acyclovir is an antiviral agent only after it is phosphorylated in infected cells by a viral-induced thymidine kinase. Acyclovir monophosphate is phosphorylated to diphosphate and triphosphate forms by cellular enzymes in the infected host cell where the drug is concentrated. Acyclovir triphosphate inactivates viral deoxyribonucleic acid polymerase.

Showing 1 - 10 of 11 results

First page disabled
Previous page disabled
1
Next page
Next page

HHS VULNERABILITY DISCLOSURE

For language access assistance, contact the NCATS Public Information Officer

National Center for Advancing Translational Sciences (NCATS),
6701 Democracy Boulevard, Bethesda MD 20892-4874 • 301-594-8966


			version 1.1