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Pneumocystis carinii

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Histamine H1 receptor

316

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Originator

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

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Leben, C.|Keitt, G.W.

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Artemisinin and derivatives, combinations

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Showing 1 - 4 of 4 results

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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.

ANTIMYCIN A1B

75G3NMU1TS

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Status:

Other

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

ATP-citrate synthase

Candida albicans

Saccharomyces cerevisiae

Pneumocystis carinii

Cytochrome b-c1 complex subunit 7

Apoptosis regulator Bcl-2

Bcl-2-like protein 1

Conditions:

Antimycin A is widely used as a piscicide in the catfish farming industry (brandname Fintrol) and has potent killing activity against insects, nematodes and fungi. Antimycin A is a potent inhibitor of ubiquinol-cytochrome C oxidoreductase (complex II...

I). By inhibiting cytochrome C reductase in the electron transport chain of mitochondria antimycin A halts respiration. It has been used to study the metabolic signature of RCD in human cultured skeletal muscle cells. The specific sites of reactive oxygen species (ROS) production in mitochondria isolated from skeletal muscle of chronic obstructive pulmonary disease and lung cancer patients, and its relationship with local oxidative stress induced by exercise have been studied using antimycin A as well. More recently, antimycin A has attracted attention as a potent and selective inhibitor of the mitochondrial anti-apoptotic proteins Bcl-2 and Bcl-xL which are over-produced in cancer cells resistant to apoptosis-inducing chemotherapy agents, so antimycin A may have a potential as anticancer drug for combination chemotherapy.

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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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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