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3

US Approved Rx

2

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Primary Target

Voltage-gated potassium channel subunit Kv1.1

3

Voltage-gated potassium channel subunit Kv1.5

3

CCRF-CEM

2

Tubulin beta chain

2

microtubule polymerization

2

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Highest Phase

Approved

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Approval Year

Unknown

3

1963

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Condition

Unknown

3

Philadelphia chromosome-negative (Ph-) acute lymphoblastic leukemia (ALL) in second or greater relapse

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Treatment Modality

Primary

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CNS Activity

CNS Non-penetrant

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Originator

Apothekernes Laboratorium For Specialpraeparat

3

Eli Lilly

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Substance Class

Chemical

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Code System

FDA UNII

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PUBCHEM

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CAS

4

EPA CompTox

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CHEBI

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ATC Level 1

ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

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ATC Level 2

ANTINEOPLASTIC AGENTS

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ATC Level 3

PLANT ALKALOIDS AND OTHER NATURAL PRODUCTS

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ATC Level 4

Vinca alkaloids and analogues

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Salts, Hydrates, Esters, etc.

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Principal Form

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Showing 1 - 5 of 5 results

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VINCRISTINE

5J49Q6B70F

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Status:

US Approved Rx (1988)

First approved in 1963

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Tubulin beta chain

microtubule polymerization

transformed cell apoptotic process

Conditions:

Philadelphia chromosome-negative (Ph-) acute lymphoblastic leukemia (ALL) in second or greater relapse

Vincristine is a vinca alkaloid antineoplastic agent used as a treatment for various cancers including breast cancer, Hodgkin's disease, Kaposi's sarcoma, and testicular cancer. The vinca alkaloids are structurally similar compounds comprised of 2 mu...

ltiringed units, vindoline and catharanthine. The vinca alkaloids have become clinically useful since the discovery of their antitumour properties in 1959. Initially, extracts of the periwinkle plant (Catharanthus roseus) were investigated because of putative hypoglycemic properties, but were noted to cause marrow suppression in rats and antileukemic effects in vitro. Vincristine binds to the microtubular proteins of the mitotic spindle, leading to crystallization of the microtubule and mitotic arrest or cell death. Vincristine has some immunosuppressant effect. The vinca alkaloids are considered to be cell cycle phase-specific. The antitumor activity of Vincristine is thought to be due primarily to inhibition of mitosis at metaphase through its interaction with tubulin. Like other vinca alkaloids, Vincristine may also interfere with: 1) amino acid, cyclic AMP, and glutathione metabolism, 2) calmodulin-dependent Ca2+-transport ATPase activity, 3) cellular respiration, and 4) nucleic acid and lipid biosynthesis.Vincristine was marketed under the brand name Oncovin, but was discontinued. In 2012 the FDA approved a Liposomal formulation of Vincristine, named MARQIBO KIT.

ROPIVACAINE, (R)-

0494L275Q6

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Status:

Other

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Voltage-gated potassium channel subunit Kv1.1

Voltage-gated potassium channel subunit Kv1.5

Conditions:

(R)-Ropivacaine (Dextroropivacaine) is a voltage-dependent potassium channel blocker with local anesthetic activity. (S)-Ropivacaine is a medication used for the production of local or regional anesthesia for surgery and for acute pain management. Ro...

pivacaine shows a difference in channel blockade between two enantiomers, and R-Ropivacaine shows greater cardiotoxicity than (S)-Ropivacaine. (R)-Ropivacaine is the impurity in commercial formulations of Ropivacaine.

VINCRISTINE SULFATE

T5IRO3534A

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Status:

US Approved Rx (1988)

First approved in 1963

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Tubulin beta chain

microtubule polymerization

transformed cell apoptotic process

Conditions:

Philadelphia chromosome-negative (Ph-) acute lymphoblastic leukemia (ALL) in second or greater relapse

Vincristine is a vinca alkaloid antineoplastic agent used as a treatment for various cancers including breast cancer, Hodgkin's disease, Kaposi's sarcoma, and testicular cancer. The vinca alkaloids are structurally similar compounds comprised of 2 mu...

ltiringed units, vindoline and catharanthine. The vinca alkaloids have become clinically useful since the discovery of their antitumour properties in 1959. Initially, extracts of the periwinkle plant (Catharanthus roseus) were investigated because of putative hypoglycemic properties, but were noted to cause marrow suppression in rats and antileukemic effects in vitro. Vincristine binds to the microtubular proteins of the mitotic spindle, leading to crystallization of the microtubule and mitotic arrest or cell death. Vincristine has some immunosuppressant effect. The vinca alkaloids are considered to be cell cycle phase-specific. The antitumor activity of Vincristine is thought to be due primarily to inhibition of mitosis at metaphase through its interaction with tubulin. Like other vinca alkaloids, Vincristine may also interfere with: 1) amino acid, cyclic AMP, and glutathione metabolism, 2) calmodulin-dependent Ca2+-transport ATPase activity, 3) cellular respiration, and 4) nucleic acid and lipid biosynthesis.Vincristine was marketed under the brand name Oncovin, but was discontinued. In 2012 the FDA approved a Liposomal formulation of Vincristine, named MARQIBO KIT.

ROPIVACAINE HYDROCHLORIDE MONOHYDRATE, (R)-

L3PZV0QTF5

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Status:

Other

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Voltage-gated potassium channel subunit Kv1.1

Voltage-gated potassium channel subunit Kv1.5

Conditions:

(R)-Ropivacaine (Dextroropivacaine) is a voltage-dependent potassium channel blocker with local anesthetic activity. (S)-Ropivacaine is a medication used for the production of local or regional anesthesia for surgery and for acute pain management. Ro...

pivacaine shows a difference in channel blockade between two enantiomers, and R-Ropivacaine shows greater cardiotoxicity than (S)-Ropivacaine. (R)-Ropivacaine is the impurity in commercial formulations of Ropivacaine.

ROPIVACAINE HYDROCHLORIDE, (R)-

MI262Q4RJI

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Search for Structure

Status:

Other

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Voltage-gated potassium channel subunit Kv1.1

Voltage-gated potassium channel subunit Kv1.5

Conditions:

(R)-Ropivacaine (Dextroropivacaine) is a voltage-dependent potassium channel blocker with local anesthetic activity. (S)-Ropivacaine is a medication used for the production of local or regional anesthesia for surgery and for acute pain management. Ro...

pivacaine shows a difference in channel blockade between two enantiomers, and R-Ropivacaine shows greater cardiotoxicity than (S)-Ropivacaine. (R)-Ropivacaine is the impurity in commercial formulations of Ropivacaine.

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