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Toltrazuril (sulfone)

(CAS: 69004-04-2)

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Background Information of Toltrazuril (sulfone)

Toltrazuril sulfone is an antiprotozoal agent that acts upon Coccidia parasites. IC50 Value: Target: Antiparasitic Ponazuril (INN, Toltrazuril sulfone), sold by the Bayer Corporation under the trade name Marquis, is a drug currently approved for the treatment of equine protozoal myeloencephalitis in horses, caused by Sarcocystis neurona.

Solubility of Toltrazuril (sulfone)

Solubility Sources

Storage Condition of Toltrazuril (sulfone)

Storage Condition Sources

MSDS Information

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Quality Control and Spectral Data

QC Reports Sources

Mechanism and Indications

Signaling Pathways Anti-infection
Target Parasite
Research Area Infection
Indications

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
Toltrazuril (sulfone) - Not Found
Toltrazuril (sulfone) - No Development Reported

Chemical Information

M.Wt Formula CAS No. Synonyms
457.38 C18H14F3N3O6S 69004-04-2 Ponazuril; 1-methyl-3-(3-methyl-4-(4-((trifluoromethyl)sulfonyl)phenoxy)phenyl)-1,3,5-triazinane-2,4,6-trione

Structure Information of Toltrazuril (sulfone)

Smiles O=S(C1=CC=C(C=C1)OC2=C(C=C(C=C2)N3C(N(C(NC3=O)=O)C)=O)C)(C(F)(F)F)=O
InChI InChI=1S/C18H14F3N3O6S/c1-10-9-11(24-16(26)22-15(25)23(2)17(24)27)3-8-14(10)30-12-4-6-13(7-5-12)31(28,29)18(19,20)21/h3-9H,1-2H3,(H,22,25,26)

Related Products

Other Form Products of Toltrazuril (sulfone)

Name CAS Formula Suppliers
Toltrazuril 69004-03-1 C18H14F3N3O4S 20

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Chemical and Physical Properties

Appearance:White to off-white Solid Melting point:
Boiling point: Flash Point:
Water Solubility: Solubility:Soluble in DMSO
Density: Merck:
BRN: Refractive Index:
Vapour: EINECS:
Optical Rotation: alpha:

Reference

[1].Pharmacokinetics of ponazuril after oral administration to healthy Ilamas (Lama glama) By Prado, Maria E.; Ryman, Josiah T.; Boileau, Melanie J.; Martin-Jimenez, Tomas; Meibohm, Bernd From American Journal of Veterinary Research (2011), 72(10), 1386-1389
To determine the pharmacokinetics after oral administration of a single dose of ponazuril to healthy llamas.Animals-6 healthy adult llamas. Procedures-Ponazuril (20 mg/kg) was administered once orally to 6 llamas (day 0). Blood samples were obtained on days 0, 0.5, 1, 2, 3, 4, 5, 6, 7, 9, 11, 14, 21, 28, 35, 42, and 49. Serum ponazuril concentrations were determined by use of a validated reverse-phase high-performance liquid chromatography assay with UV absorbance detection. Pharmacokinetic parameters were derived by use of a standard noncompartmental pharmacokinetic analysis. Results-Mean ± SD area under the serum concentration-time curve was 7,516 ± 2,750 homg/L, maximum serum ponazuril concentration was 23.6 ± 6.0 mg/L, and the elimination half-life was 135.5 ± 16.7 hours. ...

[2].Dirikolu L, Karpiesiuk W, Lehner AF, Tobin T. Toltrazuril sulfone sodium salt: synthesis, analytical detection, and pharmacokinetics in the horse. J Vet Pharmacol Ther. 2012 Jun;35(3):265-74. doi: 10.1111/j.1365-2885.2011.01315.x.
Toltrazuril sulfone (ponazuril) is a triazine-based antiprotozoal agent with clinical application in the treatment of equine protozoal myeloencephalomyelitis (EPM). In this study, we synthesized and determined the bioavailability of a sodium salt formulation of toltrazuril sulfone that can be used for the treatment and prophylaxis of EPM in horses. Toltrazuril sulfone sodium salt was rapidly absorbed, with a mean peak plasma concentration of 2400 ± 169 (SEM) ng/mL occurring at 8 h after oral-mucosal dosing and was about 56% bioavailable compared with the i.v. administration of toltrazuril sulfone in dimethylsulfoxide (DMSO). The relative bioavailability of toltrazuril sulfone suspended in water compared with toltrazuril sulfone sodium salt was 46%, indicating approximately 54% less oral bioavailability of this compound suspended in water. In this study, we also investigated whether this salt formulation of toltrazuril sulfone can be used as a feed additive formulation without significant reduction in oral bioavailability. Our results indicated that toltrazuril sulfone sodium salt is relatively well absorbed when administered with feed with a mean oral bioavailability of 52%. Based on these data, repeated oral administration of toltrazuril sulfone sodium salt with or without feed will yield effective plasma and cerebrospinal fluid (CSF) concentrations of toltrazuril sulfone for the treatment and prophylaxis of EPM and other protozoal diseases of horses and other species. As such, toltrazuril sulfone sodium salt has the potential to be used as feed additive formulations for both the treatment and prophylaxis of EPM and various other apicomplexan diseases.

[3].Lim JH, Kim MS, Hwang YH, Song IB, Park BK, Yun HI. Pharmacokinetics of toltrazuril and its metabolites, toltrazuril sulfoxide and toltrazuril sulfone, after a single oral administration to pigs. J Vet Med Sci. 2010 Aug;72(8):1085-7.
Toltrazuril (TZR) is a triazine-based antiprotozoal agent. Following a single oral administration of TZR at 10 and 20 mg/kg to male pigs, the mean TZR concentration in plasma peaked at 4.24 and 8.18 microg/ml at 15.0 and 12.0 hr post-dose, respectively. TZR absorbed was rapidly converted to the short-lived intermediary metabolite toltrazuril sulfoxide (TZR-SO), and then metabolized to the reactive toltrazuril sulfone (TZR-SO2). TZR-SO2 was actually more slowly eliminated, with average half-lives of 231 and 245 hr, compared with TZR (48.7 and 68.9 hr) or TZR-SO (51.9 and 53.2 hr) in the 10 and 20 mg/kg groups, respectively. This study demonstrates that TZR metabolizes to TZR-SO2 having a long-terminal half-life, enabling the persistent clinical efficacy in the treatment of I. suis infection. In contrast, special consideration should be given to the residual of TZR-SO2.

[4].Dirikolu L, Yohn R, Garrett EF, Chakkath T, Ferguson DC. Detection, quantifications and pharmacokinetics of toltrazuril sulfone (Ponazuril) in cattle. J Vet Pharmacol Ther. 2009 Jun;32(3):280-8.
Toltrazuril sulfone (Ponazuril) is a triazine-based anti-protozoal agent with highly specific actions against apicomplexan group of organisms, which are undergoing intensive investigation. Toltrazuril sulfone may have clinical application in the treatment of Neospora. caninum and other protozoal infections in cattle. To evaluate absorption, distribution, and elimination characteristics of toltrazuril sulfone in cattle, a sensitive validated quantitative high-pressure liquid chromatography method for toltrazuril sulfone in bovine biological fluids was developed. After a single oral dose of toltrazuril sulfone at 5 mg/kg (as 150 mg/g of Marquis; Bayer HealthCare, Shawnee Mission, KS, USA), samples from six cows showed good plasma concentrations of toltrazuril sulfone, which peaked at 4821 ng/mL +/- 916 (SD) at 48 h postadministration. Thereafter, plasma concentration declined to 1950 ng/mL +/- 184 (SD) at 192 h after administration with an average plasma elimination half-life of approximately 58 h. Following oral dose of toltrazuril sulfone, the observed peak plasma concentrations were in relatively close agreement ranging from the lowest 3925 ng/mL to the highest of 6285 ng/mL with the mean peak plasma concentration being 4821 ng/mL. This study shows that toltrazuril sulfone is relatively well absorbed after oral dose in cattle. These results are therefore entirely consistent with and support the reported clinical efficacy of toltrazuril sulfone in the treatment of experimentally induced clinical cases of N. caninum and other protozoal-mediated bovine diseases.

[5].Dirikolu L, Karpiesiuk W, Lehner AF, Hughes C, Granstrom DE, Tobin T. Synthesis and detection of toltrazuril sulfone and its pharmacokinetics in horses following administration in dimethylsulfoxide. J Vet Pharmacol Ther. 2009 Aug;32(4):368-78.
Triazine-based antiprotozoal agents are known for their lipophylic characteristics and may therefore be expected to be well absorbed following oral administration. However, although an increase in lipid solubility generally increases the absorption of chemicals, extremely lipid-soluble chemicals may dissolve poorly in gastrointestinal (GI) fluids, and their corresponding absorption and bioavailability would be low. Also, if the compound is administered in solid form and is relatively insoluble in GI fluids, it is likely to have limited contact with the GI mucosa, and therefore, its rate of absorption will be low. Based on the above considerations, we sought a solvent with low or no toxicity that would maintain triazine agents in solution. As the oral route is most preferred for daily drug therapy, such a solvent would allow an increased rate of absorption following oral administration. In present study, it was demonstrated that dimethylsulfoxide (DMSO) increased the oral bioavailability of toltrazuril sulfone (Ponazuril) threefold, relative to oral administrations of toltrazuril sulfone suspended in water. The cross-over study of toltrazuril sulfone formulated in DMSO indicated that the absolute oral bioavailability of toltrazuril sulfone in DMSO is 71%. The high bioavailability of the DMSO-preparation suggests that its daily oral administration will routinely yield effective plasma and cerebral spinal fluid (CSF) concentrations in all horses treated. Also, this improved formulation would allow clinicians to administer loading doses of toltrazuril sulfone in acute cases of Equine Protozoal Myeloencephalitis. Another option would involve administration of toltrazuril sulfone in DMSO mixed with feed (1.23 kg daily dose) meeting the US Food and Drug Administration (FDA) recommendations for the levels of DMSO permissible in pharmaceutical preparations.

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