Delamanid
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| Surname | Delamanid | |||||||||||||||
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| Molecular formula | C 25 H 25 F 3 N 4 O 6 | |||||||||||||||
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| Molar mass | 534.49 g · mol -1 | |||||||||||||||
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| As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions . | ||||||||||||||||
Delamanid (trade name Deltyba , manufacturer Otsuka Pharmaceutical ) is a drug from the group of dihydro-nitroimidazooxazoles that is used in the treatment of multi-drug-resistant tuberculosis .
field of use
On April 28, 2014, the European Commission approved Delamanid as Deltyba for the treatment of multidrug- resistant tuberculosis throughout the European Union . In the EU, Deltyba has the status of an orphan drug . It is used when the standard drugs isoniazid (INH), rifampicin (RMP), ethambutol (EMB), pyrazinamide (PZA), and streptomycin (SM) fail.
The active ingredient was first described in 2003 under the development code OPC-67683 .
Mechanism of action
Delamanid disrupts the cell wall structure by inhibiting the biosynthesis of mycolic acids ( IC 50 = 0.036 μg / mL or 0.021 μg / mL).
Interactions
Delamanid interacts with strong inducers of the liver enzyme cytochrome P450 3A4 , for example carbamazepine , as well as with other drugs that increase the QT time .
Absorption and distribution in the body
After oral intake, the maximum concentration is reached after 4–5 hours. The half-life after the end of the intake is 38 hours. After 10-14 days, steady state (equilibrium concentration) is reached.
See also
Individual evidence
- ↑ This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.
- ↑ a b entry on Delamanid. In: Römpp Online . Georg Thieme Verlag, accessed on May 19, 2015.
- ↑ Summary of the EPAR for the public. EMA, April 2014, accessed April 4, 2017 . , EU / 1/13/875, accessed on May 11, 2020.
- ↑ Union Register of medicinal products for human use - Deltyba , EU / 1/13/875 , accessed on May 12, 2020.
- ↑ Medscape Germany: Multi-resistant tuberculosis: two new active ingredients soon approved in the EU? , January 16, 2014.
- ↑ Makoto Matsumoto, Hiroyuki Hashizume, Tatsuo Tomishige, Masanori Kawasaki, Hidetsugu Tsubouchi, Hirofumi Sasaki, Yoshihiko Shimokawa, Makoto Komatsu: OPC-67683, a Nitro-Dihydro-Imidazooxazole Derivative with Promice Action against Tuberculosis Mice . In: PLoS Medicine . tape 3 , no. 11 , 2006, p. e466 , doi : 10.1371 / journal.pmed.0030466 (English).
- ↑ D. Biermann: EU approval of Delamanid against multiresistant tuberculosis , Pharmazeutische Zeitung, May 14, 2014.
- ↑ AS Xavier, M. Lakshmanan: Delamanid: A new armor in combating drug-resistant tuberculosis. In: Journal of Pharmacology & Pharmacotherapeutics . Volume 5, number 3, July 2014, pp. 222-224, doi: 10.4103 / 0976-500X.136121 , PMID 25210407 , PMC 4156838 (free full text).
