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| Targets |
Artefenomel targets the malaria parasite Plasmodium falciparum. Its mechanism involves alkylating parasite proteins. The compound is active against various strains, including 3D7, Cam3.II, and Cam3.II_rev, with LC50s of 8.7, 4.4, and 6.1 nM, respectively.
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| ln Vitro |
Proteins from Plasmodium falciparum are alkylated by artefenomel (OZ439) (10 μg/mL, 2 h) [1]. At dosages up to 300 μM, artefenomel (0.3-300 μM) decreases ACE2 expression in Vero cells in a dose-dependent manner without causing any cytotoxicity [2]. With an IC50 of 2.9 μM, artefenomel (33-100 μM) suppresses SARS-CoV-2 in a dose-dependent manner and entirely eliminates virus-induced CPE [2]. In pregnant Crl:CD(SD)BR rat embryos, artefenomel (0–10 µg/mL) damages red blood cells and causes anemia, which causes histological alterations (cell death) and macroscopic abnormalities [3].
Artefenomel shows potent in vitro activity against P. falciparum with IC50 values of 2.0 nM (K1 strain) and 3.2 nM (NF54 strain). It decreases ACE2 expression in Vero cells in a dose-dependent manner without cytotoxicity at concentrations up to 300 μM. It suppresses SARS-CoV-2 with an IC50 of 2.9 μM. |
| ln Vivo |
In vivo efficacy has been demonstrated in P. berghei mouse models. Artefenomel is an orally active antimalarial, but detailed in vivo study protocols are not specified in the available literature. Its anti-viral effect against SARS-CoV-2 has also been reported.
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| Enzyme Assay |
The antimalarial activity of Artefenomel is assessed in cell-free systems by measuring its ability to alkylate proteins from P. falciparum. This assay involves treating parasite proteins with the compound and analyzing the resulting alkylation.
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| Cell Assay |
Cell Viability Assay[3]
Cell Types: Embryos from pregnant Crl:CD(SD)BR rats Tested Concentrations: 0.1, 1, 2, 5, 7.5 and 10 µg/mL Incubation Duration: Experimental Results: demonstrated slightly shortened or slightly delayed tail Telencephalic vesicle loss occurs at 5 μg/mL, diminished circulating red blood cell numbers occur at 7.5 μg/mL, and cardiac arrhythmias occur at 10 μg/mL. The antiplasmodial activity is evaluated in vitro using P. falciparum cultures. The compound's potency is determined by measuring its IC50 or LC50 values against different parasite strains. Cytotoxicity is assessed in mammalian cell lines like Vero cells. |
| Animal Protocol |
In vivo antimalarial efficacy is typically evaluated in mouse models infected with P. berghei. While specific protocols are not detailed, standard models involve oral administration of the compound and monitoring parasitemia and survival rates.
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| ADME/Pharmacokinetics |
Artefenomel is an orally bioavailable compound. As a synthetic ozonide, it is designed to have a favorable pharmacokinetic profile, including good oral bioavailability and a long half-life, which are typical of the artemisinin-like compounds.
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| Toxicity/Toxicokinetics |
Specific toxicity data is not provided in the available literature. However, developmental toxicity has been observed in rat embryos, where it caused histological alterations and macroscopic abnormalities at concentrations of 0.1–10 µg/mL.
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| References |
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| Additional Infomation |
Artefenomel has been studied for its use in the treatment of malaria.
Artefenomel (OZ439) is a leading next-generation antimalarial drug candidate. Its development is aimed at overcoming the limitations of current artemisinin-based therapies, such as poor oral bioavailability and short half-lives. It has also shown potential as an antiviral agent against SARS-CoV-2. |
| Molecular Formula |
C28H39NO5
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|---|---|
| Molecular Weight |
469.612968683243
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| Exact Mass |
469.283
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| CAS # |
1029939-86-3
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| Related CAS # |
1029939-86-3;1029939-87-4 (mesylate);1310917-29-3;
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| PubChem CID |
24999143
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| Appearance |
White to off-white solid powder
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| LogP |
4.82
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
34
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| Complexity |
680
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
XLCNVWUKICLURR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H39NO5/c1-3-26(31-14-11-29-9-12-30-13-10-29)4-2-22(1)23-5-7-27(8-6-23)32-28(34-33-27)24-16-20-15-21(18-24)19-25(28)17-20/h1-4,20-21,23-25H,5-19H2
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~4.2 mg/mL (~8.94 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1294 mL | 10.6471 mL | 21.2943 mL | |
| 5 mM | 0.4259 mL | 2.1294 mL | 4.2589 mL | |
| 10 mM | 0.2129 mL | 1.0647 mL | 2.1294 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02083380 | Completed | Drug: Artefenomel 800mg: piperaquine 640mg Drug: Artefenomel 800mg: piperaquine 960mg Drug: Artefenomel 800mg: piperaquine 1440mg |
Uncomplicated Plasmodium Falciparum Malaria | Medicines for Malaria Venture | 2014-07 | Phase 2 Phase 3 |
| NCT03660839 | Completed | Drug: Artefenomel (OZ439) Drug: Ferroquine (SSR97193) |
Plasmodium Falciparum Infection | Sanofi | 2018-09-11 | Phase 2 |
| NCT03542149 | Completed | Drug: 480 mg Piperaquine phosphate Drug: 640 mg Piperaquine phosphate Drug: 200 mg OZ 439 |
Malaria | Medicines for Malaria Venture | 2018-04-23 | Phase 1 |
| NCT02573857 | Terminated | Drug: DSM265 Drug: OZ439 |
Malaria | Medicines for Malaria Venture | 2015-10 | Phase 1 Phase 2 |
| NCT01213966 | Completed | Drug: OZ439 | Malaria, Falciparum Malaria, Vivax |
Medicines for Malaria Venture | 2010-10 | Phase 2 |
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