Cadazolid
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MedKoo CAT#: 319542

CAS#: 1025097-10-2

Description: Cadazolid, also known ACT-179811, is a novel fluoroquinolone-oxazolidinone antibiotic and a protein synthesis inhibitor. Cadazolid may be potentially useful for the treatment of Clostridium difficile infection. Cadazolid exhibits potent in vitro activity against Clostridium difficile, including the epidemic BI/NAP1/027 strain. Clostridium difficile infection (CDI), the main cause of nosocomial infectious diarrhea, results from the growth of toxin-producing C. difficile in the colon following disruption of the normal enteric microbiota, usually as a consequence of antibiotic therapy.


Price and Availability

Size
Price

50mg
USD 450
500mg
USD 2150
Size
Price

100mg
USD 850
1g
USD 3250
Size
Price

200mg
USD 1450
2g
USD 5650

Cadazolid, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 319542
Name: Cadazolid
CAS#: 1025097-10-2
Chemical Formula: C29H29F2N3O8
Exact Mass: 585.1923
Molecular Weight: 585.56
Elemental Analysis: C, 59.48; H, 4.99; F, 6.49; N, 7.18; O, 21.86


Synonym: ACT-179811; ACT 179811; ACT179811; Cadazolid.

IUPAC/Chemical Name: 1-Cyclopropyl-6-fluoro-7-[4-({2-fluoro-4-[(5R)-5-(hydroxymethyl)-2-oxo-1,3-oxazolidin-3-yl]phenoxy}methyl)-4-hydroxypiperidin-1-yl]-4-oxo-1,4-dihydroquinolin-3-carboxylic acid

InChi Key: XWFCFMXQTBGXQW-GOSISDBHSA-N

InChi Code: InChI=1S/C29H29F2N3O8/c30-21-10-19-23(33(16-1-2-16)13-20(26(19)36)27(37)38)11-24(21)32-7-5-29(40,6-8-32)15-41-25-4-3-17(9-22(25)31)34-12-18(14-35)42-28(34)39/h3-4,9-11,13,16,18,35,40H,1-2,5-8,12,14-15H2,(H,37,38)/t18-/m1/s1

SMILES Code: O=C(C1=CN(C2CC2)C3=C(C=C(F)C(N4CCC(O)(COC5=CC=C(N6C(O[C@@H](CO)C6)=O)C=C5F)CC4)=C3)C1=O)O


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


References

1: Seiler P, Enderlin-Paput M, Pfaff P, Weiss M, Ritz D, Clozel M, Locher HH. Cadazolid does not promote intestinal colonization of vancomycin-resistant enterococci in mice. Antimicrob Agents Chemother. 2015 Oct 26. pii: AAC.01923-15. [Epub ahead of print] PubMed PMID: 26503650.

2: Kern WV. [New antibacterial agents on the market and in the pipeline]. Internist (Berl). 2015 Oct 18. [Epub ahead of print] German. PubMed PMID: 26475603.

3: Gerding DN, Hecht DW, Louie T, Nord CE, Talbot GH, Cornely OA, Buitrago M, Best E, Sambol S, Osmolski JR, Kracker H, Locher HH, Charef P, Wilcox M. Susceptibility of Clostridium difficile isolates from a Phase 2 clinical trial of cadazolid and vancomycin in C. difficile infection. J Antimicrob Chemother. 2015 Oct 3. pii: dkv300. [Epub ahead of print] PubMed PMID: 26433782.

4: Gehin M, Desnica B, Dingemanse J. Minimal systemic and high faecal exposure to cadazolid in patients with severe Clostridium difficile infection. Int J Antimicrob Agents. 2015 Nov;46(5):576-81. doi: 10.1016/j.ijantimicag.2015.07.015. Epub 2015 Sep 3. PubMed PMID: 26419191.

5: Kali A, Charles MV, Srirangaraj S. Cadazolid: A new hope in the treatment of Clostridium difficile infection. Australas Med J. 2015 Aug 31;8(8):253-62. doi: 10.4066/AMJ.2015.2441. eCollection 2015. Review. PubMed PMID: 26392822; PubMed Central PMCID: PMC4560895.

6: Louie T, Nord CE, Talbot GH, Wilcox M, Gerding DN, Buitrago M, Kracker H, Charef P, Cornely OA. Multicenter, Double-Blind, Randomized, Phase 2 Study Evaluating the Novel Antibiotic Cadazolid in Patients with Clostridium difficile Infection. Antimicrob Agents Chemother. 2015 Oct;59(10):6266-73. doi: 10.1128/AAC.00504-15. Epub 2015 Jul 27. PubMed PMID: 26248357; PubMed Central PMCID: PMC4576054.

7: Rashid MU, Dalhoff A, Weintraub A, Nord CE. In vitro activity of MCB3681 against Clostridium difficile strains. Anaerobe. 2014 Aug;28:216-9. doi: 10.1016/j.anaerobe.2014.07.001. Epub 2014 Jul 10. PubMed PMID: 25016084.

8: Karpiuk I, Tyski S. Looking for the new preparations for antibacterial therapy III. New antimicrobial agents from the quinolones group in clinical trials. Przegl Epidemiol. 2013;67(3):455-60, 557-61. English, Polish. PubMed PMID: 24340560.

9: Locher HH, Caspers P, Bruyère T, Schroeder S, Pfaff P, Knezevic A, Keck W, Ritz D. Investigations of the mode of action and resistance development of cadazolid, a new antibiotic for treatment of Clostridium difficile infections. Antimicrob Agents Chemother. 2014;58(2):901-8. doi: 10.1128/AAC.01831-13. Epub 2013 Nov 25. PubMed PMID: 24277035; PubMed Central PMCID: PMC3910891.

10: Locher HH, Seiler P, Chen X, Schroeder S, Pfaff P, Enderlin M, Klenk A, Fournier E, Hubschwerlen C, Ritz D, Kelly CP, Keck W. In vitro and in vivo antibacterial evaluation of cadazolid, a new antibiotic for treatment of Clostridium difficile infections. Antimicrob Agents Chemother. 2014;58(2):892-900. doi: 10.1128/AAC.01830-13. Epub 2013 Nov 25. PubMed PMID: 24277020; PubMed Central PMCID: PMC3910819.

11: Chilton CH, Crowther GS, Baines SD, Todhunter SL, Freeman J, Locher HH, Athanasiou A, Wilcox MH. In vitro activity of cadazolid against clinically relevant Clostridium difficile isolates and in an in vitro gut model of C. difficile infection. J Antimicrob Chemother. 2014 Mar;69(3):697-705. doi: 10.1093/jac/dkt411. Epub 2013 Oct 14. PubMed PMID: 24128668.

12: Baldoni D, Gutierrez M, Timmer W, Dingemanse J. Cadazolid, a novel antibiotic with potent activity against Clostridium difficile: safety, tolerability and pharmacokinetics in healthy subjects following single and multiple oral doses. J Antimicrob Chemother. 2014 Mar;69(3):706-14. doi: 10.1093/jac/dkt401. Epub 2013 Oct 8. PubMed PMID: 24106141.

13: Rashid MU, Lozano HM, Weintraub A, Nord CE. In vitro activity of cadazolid against Clostridium difficile strains isolated from primary and recurrent infections in Stockholm, Sweden. Anaerobe. 2013 Apr;20:32-5. doi: 10.1016/j.anaerobe.2013.02.003. Epub 2013 Feb 26. PubMed PMID: 23454525.