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Plasmodium yoelii

3

Histamine H1 receptor

316

Dopamine D2 receptor

311

DNA

282

Serotonin 2a (5-HT2a) receptor

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US Approved Rx

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2020

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Breast cancer

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Cervical cancer

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Hepatocellular carcinoma

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Malaria

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Primary

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CNS Penetrant

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Originator

Chongqing Holley|Medicines for Malaria Venture|Sigma-tau|University of Oxford

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Chemical

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ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS

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ANTIMALARIALS

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ATC Level 4

Artemisinin and derivatives, combinations

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Artemisinin and derivatives, plain

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Salts, Hydrates, Esters, etc.

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.ALPHA.-DIHYDROARTEMISININ

X0UIV26ABX

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Status:

US Approved Rx (2020)

First approved in 2020

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Plasmodium falciparum

Pneumocystis carinii

Plasmodium berghei

Plasmodium yoelii

Sodium/potassium-transporting ATPase subunit alpha-1

Plasmodium falciparum

Plasmodium falciparum

Conditions:

Hepatocellular carcinoma

Colorectal cancer

Cervical cancer

Schistosoma mansoni infection

Plasmodium falciparum malaria

Plasmodium falciparum malaria

Artenimol (dihydroartemisinin) is a derivate of antimalarial compound artemisinin. Artenimol (dihydroartemisinin) is able to reach high concentrations within the parasitized erythrocytes. Its endoperoxide bridge is thought to be essential for its ant...

imalarial activity, causing free-radical damage to parasite membrane systems including: • Inhibition of falciparum sarcoplasmic-endoplasmic reticulum calcium ATPase, • Interference with mitochondrial electron transport • Interference with parasite transport proteins • Disruption of parasite mitochondrial function. Dihydroartemisinin in combination with piperaquine tetraphosphate (Eurartesim, EMA-approved in 2011) is indicated for the treatment of uncomplicated Plasmodium falciparum malaria. The formulation meets WHO recommendations, which advise combination treatment for Plasmodium falciparum malaria to reduce the risk of resistance development, with artemisinin-based preparations regarded as the ‘policy standard’. However, experimental testing demonstrates that, due to its intrinsic chemical instability, dihydroartemisinin is not suitable to be used in pharmaceutical formulations. In addition, data show that the currently available dihydroartemisinin preparations fail to meet the internationally accepted stability requirements.

SODIUM ARTESUNATE

CN5E49Z611

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Status:

US Approved Rx (2020)

First approved in 2020

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Plasmodium falciparum

Pneumocystis carinii

Plasmodium berghei

Plasmodium yoelii

Sodium/potassium-transporting ATPase subunit alpha-1

Plasmodium falciparum

Plasmodium falciparum

Conditions:

Hepatocellular carcinoma

Colorectal cancer

Cervical cancer

Schistosoma mansoni infection

Plasmodium falciparum malaria

Plasmodium falciparum malaria

Artenimol (dihydroartemisinin) is a derivate of antimalarial compound artemisinin. Artenimol (dihydroartemisinin) is able to reach high concentrations within the parasitized erythrocytes. Its endoperoxide bridge is thought to be essential for its ant...

imalarial activity, causing free-radical damage to parasite membrane systems including: • Inhibition of falciparum sarcoplasmic-endoplasmic reticulum calcium ATPase, • Interference with mitochondrial electron transport • Interference with parasite transport proteins • Disruption of parasite mitochondrial function. Dihydroartemisinin in combination with piperaquine tetraphosphate (Eurartesim, EMA-approved in 2011) is indicated for the treatment of uncomplicated Plasmodium falciparum malaria. The formulation meets WHO recommendations, which advise combination treatment for Plasmodium falciparum malaria to reduce the risk of resistance development, with artemisinin-based preparations regarded as the ‘policy standard’. However, experimental testing demonstrates that, due to its intrinsic chemical instability, dihydroartemisinin is not suitable to be used in pharmaceutical formulations. In addition, data show that the currently available dihydroartemisinin preparations fail to meet the internationally accepted stability requirements.

ARTESUNATE

60W3249T9M

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Search for Structure

Status:

US Approved Rx (2020)

First approved in 2020

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Plasmodium falciparum

Pneumocystis carinii

Plasmodium berghei

Plasmodium yoelii

Sodium/potassium-transporting ATPase subunit alpha-1

Plasmodium falciparum

Plasmodium falciparum

Conditions:

Hepatocellular carcinoma

Colorectal cancer

Cervical cancer

Schistosoma mansoni infection

Plasmodium falciparum malaria

Plasmodium falciparum malaria

Artenimol (dihydroartemisinin) is a derivate of antimalarial compound artemisinin. Artenimol (dihydroartemisinin) is able to reach high concentrations within the parasitized erythrocytes. Its endoperoxide bridge is thought to be essential for its ant...

imalarial activity, causing free-radical damage to parasite membrane systems including: • Inhibition of falciparum sarcoplasmic-endoplasmic reticulum calcium ATPase, • Interference with mitochondrial electron transport • Interference with parasite transport proteins • Disruption of parasite mitochondrial function. Dihydroartemisinin in combination with piperaquine tetraphosphate (Eurartesim, EMA-approved in 2011) is indicated for the treatment of uncomplicated Plasmodium falciparum malaria. The formulation meets WHO recommendations, which advise combination treatment for Plasmodium falciparum malaria to reduce the risk of resistance development, with artemisinin-based preparations regarded as the ‘policy standard’. However, experimental testing demonstrates that, due to its intrinsic chemical instability, dihydroartemisinin is not suitable to be used in pharmaceutical formulations. In addition, data show that the currently available dihydroartemisinin preparations fail to meet the internationally accepted stability requirements.

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