Delamanid

Delamanid
Clinical data
Trade names Deltyba
Synonyms OPC-67683
AHFS/Drugs.com International Drug Names
License data
Routes of
administration		 by mouth (film-coated tablets)
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Protein binding ≥99.5%
Metabolism in plasma by albumin, in liver
by CYP3A4 (to a lesser extent)
Elimination half-life 30–38 hours
Excretion not excreted in urine[1]
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
Formula C25H25F3N4O6
Molar mass 534.48 g/mol
3D model (JSmol)

Delamanid, sold under the brand name Deltyba, is a medication used to treat tuberculosis.[2] Specifically it is used, along with other antituberculosis medications, for active multidrug-resistant tuberculosis.[2] It is taken by mouth.[2]

Common side effects include headache, dizziness, and nausea.[3] Other side effects include QT prolongation.[2] It has not been studied in pregnancy as of 2016.[4] Delamanid works by blocking the manufacture of mycolic acids thus destabilising the bacterial cell wall.[5] It is in the nitroimidazole class of medications.[6]

Delamanid was approved for medical use in 2014 in Europe, Japan, and South Korea.[7] It is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system.[8] As of 2016 the Stop TB Partnership had an agreement to get the medication for 1,700 USD per six month for use in more than 100 countries.[9]

Medical uses

Delamanid is used, along with other antituberculosis medications, for active multidrug-resistant tuberculosis.[2]

Adverse effects

Common side effects include headache, dizziness, and nausea.[3] Other side effects include QT prolongation.[2] It has not been studied in pregnancy as of 2016.[4]

Interactions

Delamanid is metabolised by the liver enzyme CYP3A4; therefore strong inducers of this enzyme can reduce its effectiveness.[10]

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.[11][12]

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.[13]

Society and culture

The medication was not readily available globally as of 2015. It was believed that pricing will be similar to bedaquiline, which for six months is approximately 900 USD in low income countries, 3,000 USD in middle income countries, and 30,000 USD in high income countries.[2] As of 2016 the Stop TB Partnership had an agreement to get the medication for 1,700 USD per six month.[9]

See also

References

  1. ↑ "Deltyba (delamanid): Summary of Product Characteristics. 5.2. Pharmacokinetic Properties" (PDF). Otsuka Novel Products GmbH. p. 10. Archived (PDF) from the original on 17 August 2016. Retrieved 9 July 2016.
  2. 1 2 3 4 5 6 7 The selection and use of essential medicines: Twentieth report of the WHO Expert Committee 2015 (including 19th WHO Model List of Essential Medicines and 5th WHO Model List of Essential Medicines for Children) (PDF). WHO. 2015. pp. 29–31. ISBN 9789240694941. Archived (PDF) from the original on 2016-12-20.
  3. 1 2 Side Effects of Drugs Annual: A Worldwide Yearly Survey of New Data in Adverse Drug Reactions. Elsevier. 2016. p. 284. ISBN 9780444638892. Archived from the original on 2016-12-20.
  4. 1 2 Cohen, Jonathan; Powderly, William G.; Opal, Steven M. (2016). Infectious Diseases. Elsevier Health Sciences. p. 284. ISBN 9780702063381. Archived from the original on 2016-12-20.
  5. ↑ Blair, HA; Scott, LJ (January 2015). "Delamanid: a review of its use in patients with multidrug-resistant tuberculosis". Drugs. 75 (1): 91–100. doi:10.1007/s40265-014-0331-4. PMID 25404020.
  6. ↑ Cavalcanti, Milena de Paiva; Pereira, Valeria Rego Alves; Dessein, Alain Joseph Jacques (2017). Tropical Diseases: An Overview of Major Diseases Occurring in the Americas. Bentham Science Publishers. p. 461. ISBN 9781681085876.
  7. ↑ Fischer, Janos (2016). Successful Drug Discovery. John Wiley & Sons. p. 139. ISBN 9783527341153. Archived from the original on 2016-12-20.
  8. ↑ "WHO Model List of Essential Medicines (19th List)" (PDF). World Health Organization. April 2015. Archived (PDF) from the original on 13 December 2016. Retrieved 8 December 2016.
  9. 1 2 "Stop TB Partnership | "Stop TB Partnership's Global Drug Facility jumpstarts access to new drugs for MDR-TB with innovative public-private partnerships". www.stoptb.org. Archived from the original on 16 January 2017. Retrieved 15 January 2017.
  10. ↑ Pharmazeutische Zeitung: Delamanid: Neuer Wirkstoff gegen multiresistente TB Archived 2015-09-24 at the Wayback Machine., 9 May 2014. (in German)
  11. ↑ H. Spreitzer (18 February 2013). "Bedaquilin". Österreichische Apothekerzeitung (in German) (4/2013): 22.
  12. ↑ 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.
  13. ↑ Drug Discovery & Development. EMA Recommends Two New Tuberculosis Treatments. Archived 2013-12-03 at the Wayback Machine. November 22, 2013.
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