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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/07/13 02:24:31」(JST)

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Delamanid (USAN, INN) is a drug for the treatment of multi-drug-resistant tuberculosis. It works by blocking the synthesis of mycolic acids in Mycobacterium tuberculosis, the organism which causes tuberculosis, thus destabilising its cell wall.^[2]^[3]^[4] The drug is approved in the EU under the trade name Deltyba (made by Otsuka Pharmaceutical).

It is on the World Health Organization's List of Essential Medicines, the most important medications needed in a basic health system.^[5]

Adverse effects

Delamanid prolongs QT interval.^[6]

Interactions

Delamanid is metabolised by the liver enzyme CYP3A4, wherefore strong inducers of this enzyme can reduce its effectiveness.^[6]

History

In phase II clinical trials, the drug was used in combination with standard treatments, such as four or five of the drugs ethambutol, isoniazid, pyrazinamide, rifampicin, aminoglycoside antibiotics, and quinolones. Healing rates (measured as sputum culture conversion) were significantly better in patients who additionally took delamanid.^[4]^[7]

The European Medicines Agency (EMA) recommended conditional marketing authorization for delamanid in adults with multidrug-resistant pulmonary tuberculosis without other treatment options because of resistance or tolerability. The EMA considered the data show that the benefits of delamanid outweigh the risks, but that additional studies were needed on the long-term effectiveness.^[8]

References

^ "Deltyba (delamanid): Summary of Product Characteristics. 5.2. Pharmacokinetic Properties" (PDF). Otsuka Novel Products GmbH. p. 10. Retrieved 9 July 2016.
^ Matsumoto, M.; Hashizume, H.; Tomishige, T.; Kawasaki, M.; Tsubouchi, H.; Sasaki, H.; Shimokawa, Y.; Komatsu, M. (2006). "OPC-67683, a Nitro-Dihydro-Imidazooxazole Derivative with Promising Action against Tuberculosis in Vitro and in Mice". PLoS Medicine 3 (11): e466. doi:10.1371/journal.pmed.0030466. PMC 1664607. PMID 17132069.
^ Skripconoka, V.; Danilovits, M.; Pehme, L.; Tomson, T.; Skenders, G.; Kummik, T.; Cirule, A.; Leimane, V.; Kurve, A.; Levina, K.; Geiter, L. J.; Manissero, D.; Wells, C. D. (2012). "Delamanid Improves Outcomes and Reduces Mortality for Multidrug-Resistant Tuberculosis". European Respiratory Journal 41 (6): 1393–1400. doi:10.1183/09031936.00125812. PMC 3669462. PMID 23018916.
^ ^a ^b H. Spreitzer (18 February 2013). "Neue Wirkstoffe – Bedaquilin und Delamanid". Österreichische Apothekerzeitung (in German) (4/2013): 22.
^ "WHO Model List of EssentialMedicines" (PDF). World Health Organization. October 2013. Retrieved 22 April 2014.
^ ^a ^b Pharmazeutische Zeitung: Delamanid: Neuer Wirkstoff gegen multiresistente TB, 9 May 2014. (German)
^ Gler, M. T.; Skripconoka, V.; Sanchez-Garavito, E.; Xiao, H.; Cabrera-Rivero, J. L.; Vargas-Vasquez, D. E.; Gao, M.; Awad, M.; Park, S. K.; Shim, T. S.; Suh, G. Y.; Danilovits, M.; Ogata, H.; Kurve, A.; Chang, J.; Suzuki, K.; Tupasi, T.; Koh, W. J.; Seaworth, B.; Geiter, L. J.; Wells, C. D. (2012). "Delamanid for Multidrug-Resistant Pulmonary Tuberculosis". New England Journal of Medicine 366 (23): 2151–2160. doi:10.1056/NEJMoa1112433. PMID 22670901.
^ Drug Discovery & Development. EMA Recommends Two New Tuberculosis Treatments. November 22, 2013.

UpToDate Contents

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1. 薬剤耐性結核の診断、治療、および予防 diagnosis treatment and prevention of drug resistant tuberculosis
2. 広範囲薬剤耐性結核の疫学 epidemiology of extensively drug resistant tuberculosis

English Journal

Determination of MIC Distribution and Epidemiological Cut-Off Values for Bedaquiline and Delamanid in Mycobacterium tuberculosis Using MGIT 960/TB eXiST.

Keller PM1, Hömke R2, Ritter C2, Valsesia G3, Bloemberg GV3, Böttger EC2.
Antimicrobial agents and chemotherapy.Antimicrob Agents Chemother.2015 May 4. pii: AAC.00614-15. [Epub ahead of print]
Bedaquiline and delamanid have recently been approved by the regulatory authorities for treatment of multidrug-resistant tuberculosis (MDR-TB). Antimicrobial susceptibility testing is not established for either substance. On the basis of MGIT 960/TB eXiST we determined a mean bedaquiline MIC of wild
PMID 25941226

Long-term mortality assessment of multidrug-resistant tuberculosis patients treated with delamanid.

Wells CD1, Gupta R2, Hittel N3, Geiter LJ2.
The European respiratory journal.Eur Respir J.2015 May;45(5):1498-501. doi: 10.1183/09031936.00176314. Epub 2015 Feb 19.
PMID 25700385

[New Drugs for the Treatment of Multidrug-resistant Tuberculosis (MDR-TB)].

Schaberg T1, Otto-Knapp R2, Bauer T2.
Pneumologie (Stuttgart, Germany).Pneumologie.2015 May;69(5):282-6. doi: 10.1055/s-0034-1391920. Epub 2015 May 13.
This article summarizes the state of development of new drugs for the treatment of multidrug-resistant tuberculosis. We focused on delamanid, bedaquiline, pretomanid, SQ 109 and sutezolid. © Georg Thieme Verlag KG Stuttgart · New York.
PMID 25970122

Japanese Journal

THE USE OF DELAMANID

TheTreatmentCommitteeoftheJapaneseSocietyforTuberculosis
結核 90(1), 7-10, 2015-01
NAID 40020328632

Delamanid Does Not Inhibit or Induce Cytochrome P450 Enzymes in Vitro

Shimokawa Yoshihiko,Sasahara Katsunori,Yoda Noriaki [他]
Biological & pharmaceutical bulletin 37(11), 1727-1735, 2014-11
NAID 40020248043

Delamanid Does Not Inhibit or Induce Cytochrome P450 Enzymes in Vitro

Shimokawa Yoshihiko,Sasahara Katsunori,Yoda Noriaki,Mizuno Katsuhiko,Umehara Ken
Biological and Pharmaceutical Bulletin 37(11), 1727-1735, 2014
… Delamanid is a new drug for the treatment of multidrug-resistant tuberculosis. … The ability of delamanid to inhibit or induce CYP enzymes was investigated in vitro using human liver microsomes or human hepatocytes. … Delamanid (100 µM) had little potential for mechanism-based inactivation on eight CYP isoforms (CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and CYP3A4). …
NAID 130004703892

Related Pictures

Delamanid tuberculosis drug molecule - Stock Image F011/1518 - Science Photo Library Delamanid - Use, dose, trials, side effects & availability Delamanid tuberculosis drug - Stock Image F007/0139 - Science Photo Library Metabolic Mechanism of Delamanid, a New Anti-Tuberculosis Drug, in Human Plasma | Drug New drugs and regimens for TB: 2015 update - ppt video online download Delamanidイラストとクリップアート。4 Delamanidロイヤリティ Delamanid Stock Photo Images. 5 Delamanid imagenes libres de derechos y fotografias Delamanid Tuberculosis Drug Stock Illustration | Getty Images

★リンクテーブル★

リンク元

「デラマニド」

Delamanid
Systematic (IUPAC) name
	(2R)-2-Methyl-6-nitro-2-[(4-{4-[4-(trifluoromethoxy)phenoxy]-1-piperidinyl}phenoxy)methyl]-2,3-dihydroimidazo[2,1-b][1,3]oxazole
Clinical data
Trade names	Deltyba
AHFS/Drugs.com	International Drug Names
Routes of; administration	Oral (film-coated tablets)
Legal status
Legal status	℞ (Prescription only);
Pharmacokinetic data
Protein binding	≥99.5%
Metabolism	in plasma by albumin, in liver; by CYP3A4 (to a lesser extent)
Biological half-life	30–38 hours
Excretion	not excreted in urine
Identifiers
CAS Number	681492-22-8
ATC code	J04AK06 (WHO)
PubChem	CID 6480466
ChemSpider	4981055
ChEMBL	CHEMBL218650
Synonyms	OPC-67683
Chemical data
Formula	C25H25F3N4O6
Molar mass	534.48 g/mol
	SMILES FC(F)(F)Oc5ccc(OC4CCN(c3ccc(OC[C@@]2(Oc1nc(cn1C2)[N+]([O-])=O)C)cc3)CC4)cc5 ;
	InChI InChI=1S/C25H25F3N4O6/c1-24(15-31-14-22(32(33)34)29-23(31)38-24)16-35-18-4-2-17(3-5-18)30-12-10-20(11-13-30)36-19-6-8-21(9-7-19)37-25(26,27)28/h2-9,14,20H,10-13,15-16H2,1H3/t24-/m1/s1 ; Key:XDAOLTSRNUSPPH-XMMPIXPASA-N ;

　　[★]

英: delamanid
商: デルティバ
関: 抗結核薬

[1] "Deltyba (delamanid): Summary of Product Characteristics. 5.2. Pharmacokinetic Properties" (PDF). Otsuka Novel Products GmbH. p. 10. Retrieved 9 July 2016.

[2] Matsumoto, M.; Hashizume, H.; Tomishige, T.; Kawasaki, M.; Tsubouchi, H.; Sasaki, H.; Shimokawa, Y.; Komatsu, M. (2006). "OPC-67683, a Nitro-Dihydro-Imidazooxazole Derivative with Promising Action against Tuberculosis in Vitro and in Mice". PLoS Medicine 3 (11): e466. doi:10.1371/journal.pmed.0030466. PMC 1664607. PMID 17132069.

[3] Skripconoka, V.; Danilovits, M.; Pehme, L.; Tomson, T.; Skenders, G.; Kummik, T.; Cirule, A.; Leimane, V.; Kurve, A.; Levina, K.; Geiter, L. J.; Manissero, D.; Wells, C. D. (2012). "Delamanid Improves Outcomes and Reduces Mortality for Multidrug-Resistant Tuberculosis". European Respiratory Journal 41 (6): 1393–1400. doi:10.1183/09031936.00125812. PMC 3669462. PMID 23018916.

[Spreitzer-4] H. Spreitzer (18 February 2013). "Neue Wirkstoffe – Bedaquilin und Delamanid". Österreichische Apothekerzeitung (in German) (4/2013): 22.

[5] "WHO Model List of EssentialMedicines" (PDF). World Health Organization. October 2013. Retrieved 22 April 2014.

[PZ-6] Pharmazeutische Zeitung: Delamanid: Neuer Wirkstoff gegen multiresistente TB, 9 May 2014. (German)

[7] Gler, M. T.; Skripconoka, V.; Sanchez-Garavito, E.; Xiao, H.; Cabrera-Rivero, J. L.; Vargas-Vasquez, D. E.; Gao, M.; Awad, M.; Park, S. K.; Shim, T. S.; Suh, G. Y.; Danilovits, M.; Ogata, H.; Kurve, A.; Chang, J.; Suzuki, K.; Tupasi, T.; Koh, W. J.; Seaworth, B.; Geiter, L. J.; Wells, C. D. (2012). "Delamanid for Multidrug-Resistant Pulmonary Tuberculosis". New England Journal of Medicine 366 (23): 2151–2160. doi:10.1056/NEJMoa1112433. PMID 22670901.

[8] Drug Discovery & Development. EMA Recommends Two New Tuberculosis Treatments. November 22, 2013.

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delamanid