Artenimol API Manufacturers

General Description:

Artenimol, identified by CAS number 71939-50-9, is a notable compound with significant therapeutic applications. Artenimol is an artemisinin derivative and antimalarial agent used in the treatment of uncomplicated *Plasmodium falciparum* infections . It was first authorized for market by the European Medicines Agency in October 2011 in combination with as the product Eurartesim. Artemisinin combination therapy is highly effective against malaria and stongly recommended by the World Health Organization .

Indications:

This drug is primarily indicated for: For the treatment of uncomplicated *Plasmodium falciparum* infection in adults, children, and infants aged 6 months and up weighing over 5 kg . Used in combination with . Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

Artenimol undergoes metabolic processing primarily in: The primary metabolite of Artenimol is the glucuronide conjugate, α-artenimol-β-glucuronide . It is largely metabolized by UGT1A9 with some contribution by UGT2B7 . This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Absorption:

The absorption characteristics of Artenimol are crucial for its therapeutic efficacy: The reported oral bioavailability of Artenimol was reported to be 45% in healthy adults . The observed Tmax was 1-2 h This is known to increase in malaria infected patients which could be attributed to reduced metabolism by the liver or the drug's collection in infected erythrocytes. Artenimol was obeserved to have flip-flop kinetics with an overall absorption half-life of 1.04 h. When administered with food the AUC for Artenimol increases by 144%. Cmax was observed to increase by 129% but was not found to be statistically significant. Food was observed to delay Tmax by 1 h. The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Half-life:

The half-life of Artenimol is an important consideration for its dosing schedule: Artenimol was reported to have a half life of elimination of approximately 1 h . This determines the duration of action and helps in formulating effective dosing regimens.

Protein Binding:

Artenimol exhibits a strong affinity for binding with plasma proteins: Artenimol has been reported to be 44-93% bound to plasma proteins . The identity of these proteins has not been reported. This property plays a key role in the drug's pharmacokinetics and distribution within the body.

Route of Elimination:

The elimination of Artenimol from the body primarily occurs through: Artenimol is eliminated via metabolism to glucuronide conjugates . There is little data on elimination of Artenimol but elimination of unchanged artemisinin compounds in feces and urine has been reported to be negligible. Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Volume of Distribution:

Artenimol is distributed throughout the body with a volume of distribution of: Artenimol was observed to have a mean apparent volume of distribution of 0.801 L/kg in adult patients and 0.705 L/kg in pediatric patients wit *P. falciparum* malaria . This metric indicates how extensively the drug permeates into body tissues.

Clearance:

The clearance rate of Artenimol is a critical factor in determining its safe and effective dosage: Artenimol was observed to have a mean apparent clearance of 1.340 L/h/kg in adult patients and 1.450 L/h/kg in pediatric patients with *P. falciparum* malaria . It reflects the efficiency with which the drug is removed from the systemic circulation.

Pharmacodynamics:

Artenimol exerts its therapeutic effects through: Artenimol is thought to form a reactive carbon radical intermediate which kills *P. falciparum* through alkylation of a wide array of proteins. The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Artenimol functions by: Artemisinins, including Artenimol which is a major active metabolite of many artemisinins, are thought to act via a common mechanism . While the exact mechanism of action is not certain, theories exist as to how artemisinins produce their antimalarial effect. Artemisinins are believed to bind to haem within the *P. falciparum* parasite . The source of this haem varies with the life stage of the parasite. When the parasite is in the early ring stage artemisinins are believed to bind haem produced by the parasite's haem biosynthesis pathway. In later stages artemisinins likely bind to haem released by haemoglobin digestion. Once bound to haem, artemisinins are thought to undergo activation involving ferrous iron via reductive scission which splits the endoperoxide bridge to produce a reactive oxygen . This reactive oxygen is thought to undergo a subsequent intramolecular hydrogen abstraction to produce a reactive carbon radical . The carbon radical is believed to be the source of the drugs potent activity against *P. falciparum* by alkylating a wide array of protein targets . The nature and magnitude of the effect on specific protein function as a result of this alkylation is unknown. One target which has been the focus of research is the sarco/endoplasmic reticulum Ca2+ ATPase pump of *P. falciparum* . Artemisinins have been found to irreversably bind to and inhibit this protein at a binding site similar to that of Thapsigargin. The mechanism is likely the same as for other proteins, namely alkylation via the carbon radical intermediate. Artemisinins appear to preferentially collect in infected erythrocytes, concentrating the drug by several hundred-fold compared to uninfected cells . This may play a role in why little alkylation is seen in uninfected erythrocytes . This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Categories:

Artenimol is categorized under the following therapeutic classes: Anti-Infective Agents, Antimalarials, Antiparasitic Agents, Antiparasitic Products, Insecticides and Repellents, Antiprotozoals, Artemisia, Artemisinin and derivatives, Cytochrome P-450 CYP2C19 Inhibitors, Cytochrome P-450 CYP2C19 Inhibitors (weak), Cytochrome P-450 CYP2D6 Inhibitors, Cytochrome P-450 CYP2D6 Inhibitors (strength unknown), Cytochrome P-450 Enzyme Inhibitors, Free Radicals, Peroxides, Sesquiterpenes, Terpenes, UGT1A9 Substrates, UGT2B7 substrates. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.

Experimental Properties:

Further physical and chemical characteristics of Artenimol include:

• Melting Point: 164-165