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US Approved Rx

3

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Primary Target

Ferriprotoporphyrin IX

3

PfATP6, Plasmodium falciparum

3

Plasmodium berghei

3

Plasmodium falciparum

3

Toxoplasma gondii

3

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Highest Phase

Approved

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Approval Year

2009

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Condition

Cervical cancer

3

Malaria

3

Plasmodium falciparum malaria

3

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Treatment Modality

Curative

3

Primary

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CNS Activity

CNS Penetrant

3

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Originator

Li, Y<U+044E>|Yu, P.-L.|Chen, Y.-X.|Li, L.-Q.|Gai, Y.-Z.|Wang, D.-S.|Zheng, Y.-P.

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Chemical

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Code System

CAS

3

ChEMBL

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DRUG BANK

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DRUG CENTRAL

3

EPA CompTox

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ATC Level 1

ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS

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ATC Level 2

ANTIPROTOZOALS

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ATC Level 3

ANTIMALARIALS

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ATC Level 4

Artemisinin and derivatives, plain

3

Artemisinin and derivatives, combinations

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Substance Form

Salts, Hydrates, Esters, etc.

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Principal Form

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Showing 1 - 3 of 3 results

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Artenimol

6A9O50735X

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Status:

US Approved Rx (2009)

First approved in 2009

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

PfATP6, Plasmodium falciparum

Plasmodium falciparum

Toxoplasma gondii

Plasmodium berghei

Plasmodium falciparum

Ferriprotoporphyrin IX

Conditions:

Plasmodium falciparum malaria

Cervical cancer

Plasmodium falciparum malaria

Artemether is an antimalarial agent used to treat acute uncomplicated malaria. It is administered in combination with lumefantrine for improved efficacy against malaria. Artemether is rapidly metabolized into an active metabolite dihydroartemisinin (...

DHA). The antimalarial activity of artemether and DHA has been attributed to endoperoxide moiety. Artemethe involves an interaction with ferriprotoporphyrin IX (“heme”), or ferrous ions, in the acidic parasite food vacuole, which results in the generation of cytotoxic radical species. The generally accepted mechanism of action of peroxide antimalarials involves interaction of the peroxide-containing drug with heme, a hemoglobin degradation byproduct, derived from proteolysis of hemoglobin. This interaction is believed to result in the formation of a range of potentially toxic oxygen and carbon-centered radicals. Other mechanisms of action for artemether include their ability to reduce fever by production of signals to hypothalamus thermoregulatory center. Now, recent research has shown the presence of a new, previously unknown cyclooxygenase enzyme COX-3, found in the brain and spinal cord, which is selectively inhibited by artemether, and is distinct from the two already known cyclooxygenase enzymes COX-1 and COX-2. It is now believed that this selective inhibition of the enzyme COX-3 in the brain and spinal cord explains the ability of artemether in relieving pain and reducing fever which is produced by malaria. The most common adverse reactions in adults (>30%) are headache, anorexia, dizziness, asthenia, arthralgia and myalgia.

ARTEMETHER

C7D6T3H22J

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Status:

US Approved Rx (2009)

First approved in 2009

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

PfATP6, Plasmodium falciparum

Plasmodium falciparum

Toxoplasma gondii

Plasmodium berghei

Plasmodium falciparum

Ferriprotoporphyrin IX

Conditions:

Plasmodium falciparum malaria

Cervical cancer

Plasmodium falciparum malaria

Artemether is an antimalarial agent used to treat acute uncomplicated malaria. It is administered in combination with lumefantrine for improved efficacy against malaria. Artemether is rapidly metabolized into an active metabolite dihydroartemisinin (...

DHA). The antimalarial activity of artemether and DHA has been attributed to endoperoxide moiety. Artemethe involves an interaction with ferriprotoporphyrin IX (“heme”), or ferrous ions, in the acidic parasite food vacuole, which results in the generation of cytotoxic radical species. The generally accepted mechanism of action of peroxide antimalarials involves interaction of the peroxide-containing drug with heme, a hemoglobin degradation byproduct, derived from proteolysis of hemoglobin. This interaction is believed to result in the formation of a range of potentially toxic oxygen and carbon-centered radicals. Other mechanisms of action for artemether include their ability to reduce fever by production of signals to hypothalamus thermoregulatory center. Now, recent research has shown the presence of a new, previously unknown cyclooxygenase enzyme COX-3, found in the brain and spinal cord, which is selectively inhibited by artemether, and is distinct from the two already known cyclooxygenase enzymes COX-1 and COX-2. It is now believed that this selective inhibition of the enzyme COX-3 in the brain and spinal cord explains the ability of artemether in relieving pain and reducing fever which is produced by malaria. The most common adverse reactions in adults (>30%) are headache, anorexia, dizziness, asthenia, arthralgia and myalgia.

ARTEMISININ

9RMU91N5K2

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Status:

US Approved Rx (2009)

First approved in 2009

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

PfATP6, Plasmodium falciparum

Plasmodium falciparum

Toxoplasma gondii

Plasmodium berghei

Plasmodium falciparum

Ferriprotoporphyrin IX

Conditions:

Plasmodium falciparum malaria

Cervical cancer

Plasmodium falciparum malaria

Artemether is an antimalarial agent used to treat acute uncomplicated malaria. It is administered in combination with lumefantrine for improved efficacy against malaria. Artemether is rapidly metabolized into an active metabolite dihydroartemisinin (...

DHA). The antimalarial activity of artemether and DHA has been attributed to endoperoxide moiety. Artemethe involves an interaction with ferriprotoporphyrin IX (“heme”), or ferrous ions, in the acidic parasite food vacuole, which results in the generation of cytotoxic radical species. The generally accepted mechanism of action of peroxide antimalarials involves interaction of the peroxide-containing drug with heme, a hemoglobin degradation byproduct, derived from proteolysis of hemoglobin. This interaction is believed to result in the formation of a range of potentially toxic oxygen and carbon-centered radicals. Other mechanisms of action for artemether include their ability to reduce fever by production of signals to hypothalamus thermoregulatory center. Now, recent research has shown the presence of a new, previously unknown cyclooxygenase enzyme COX-3, found in the brain and spinal cord, which is selectively inhibited by artemether, and is distinct from the two already known cyclooxygenase enzymes COX-1 and COX-2. It is now believed that this selective inhibition of the enzyme COX-3 in the brain and spinal cord explains the ability of artemether in relieving pain and reducing fever which is produced by malaria. The most common adverse reactions in adults (>30%) are headache, anorexia, dizziness, asthenia, arthralgia and myalgia.

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