Inxight Drugs

Search results for "Established Pharmacologic Class [EPC]|Topoisomerase Inhibitor [EPC]" in comments (approximate match)

Showing 1 - 5 of 5 results

IRINOTECAN

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7673326042

Status:

US Approved Rx (2008)

First approved in 1996

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Conditions:

Irinotecan is an antineoplastic enzyme inhibitor primarily used in the treatment of colorectal cancer. Irinotecan is sold under the brand name Camptosar among others. CAMPTOSAR is a topoisomerase inhibitor indicated for: • First-line therapy in comb...

TOPOTECAN

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7M7YKX2N15

Status:

US Approved Rx (2010)

First approved in 1996

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Conditions:

Topotecan, a semi-synthetic derivative of camptothecin (a plant alkaloid obtained from the Camptotheca acuminata tree), is an anti-tumor drug with topoisomerase I-inhibitory activity similar to irinotecan. DNA topoisomerases are enzymes in the cell n...

ucleus that regulate DNA topology (3-dimensional conformation) and facilitate nuclear processes such as DNA replication, recombination, and repair. During these processes, DNA topoisomerase I creates reversible single-stranded breaks in double-stranded DNA, allowing intact single DNA strands to pass through the break and relieve the topologic constraints inherent in supercoiled DNA. The 3'-DNA terminus of the broken DNA strand binds covalently with the topoisomerase enzyme to form a catalytic intermediate called a cleavable complex. After DNA is sufficiently relaxed and the strand passage reaction is complete, DNA topoisomerase reattaches the broken DNA strands to form the unaltered topoisomers that allow transcription to proceed. Topotecan interferes with the growth of cancer cells, which are eventually destroyed. Since the growth of normal cells can be affected by the medicine, other effects may also occur. Unlike irinotecan, topotecan is found predominantly in the inactive carboxylate form at neutral pH and it is not a prodrug. Topotecan has the same mechanism of action as irinotecan and is believed to exert its cytotoxic effects during the S-phase of DNA synthesis. Topoisomerase I relieves torsional strain in DNA by inducing reversible single strand breaks. Topotecan binds to the topoisomerase I-DNA complex and prevents religation of these single strand breaks. This ternary complex interferes with the moving replication fork, which leads to the induction of replication arrest and lethal double-stranded breaks in DNA. As mammalian cells cannot efficiently repair these double strand breaks, the formation of this ternary complex eventually leads to apoptosis (programmed cell death). Topotecan mimics a DNA base pair and binds at the site of DNA cleavage by intercalating between the upstream (−1) and downstream (+1) base pairs. Intercalation displaces the downstream DNA, thus preventing religation of the cleaved strand. By specifically binding to the enzyme–substrate complex, Topotecan acts as an uncompetitive inhibitor. Topotecan is used for the treatment of advanced ovarian cancer in patients with disease that has recurred or progressed following therapy with platinum-based regimens. Also used as a second-line therapy for treatment-sensitive small cell lung cancer, as well as in combination with cisplatin for the treatment of stage IV-B, recurrent, or persistent cervical cancer not amenable to curative treatment with surgery and/or radiation therapy. Topotecan is sold under the trade name Hycamtin.

MITOXANTRONE

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BZ114NVM5P

Status:

US Approved Rx (2006)

First approved in 1987

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Conditions:

Mitoxantrone (NOVANTRONE) is a synthetic antineoplastic anthracenedione. Mitoxantrone, a DNA-reactive agent that intercalates into deoxyribonucleic acid (DNA) through hydrogen bonding, causes crosslinks and strand breaks. Mitoxantrone also interferes...

ETOPOSIDE

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6PLQ3CP4P3

Status:

US Approved Rx (1998)

First approved in 1983

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Conditions:

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...

TENIPOSIDE

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957E6438QA

Status:

US Previously Marketed

First approved in 1992

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Conditions:

Teniposide is an inhibitor of topoisomerase II with anti-cancer activity. The drug was approved by FDA under the name Vumon for the treatment of children with acute lymphoblastic leukemia.

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Search results for "Established Pharmacologic Class [EPC]|Topoisomerase Inhibitor [EPC]" in comments (approximate match)

IRINOTECAN

7673326042

TOPOTECAN

7M7YKX2N15

MITOXANTRONE

BZ114NVM5P

ETOPOSIDE

6PLQ3CP4P3

TENIPOSIDE

957E6438QA