Lurbinectedin

Lurbinectedin
Clinical data
Pronunciation/ˌlɜːrbɪˈnɛktɪdɪn/
LUR-bi-NEK-ti-din
Trade namesZepzelca
Other namesPM-01183
AHFS/Drugs.comProfessional Drug Facts
MedlinePlusa620049
License data
Pregnancy
category
Routes of
administration		Intravenous
Drug classAntineoplastic agent
ATC code
Legal status
Legal status
Identifiers
  • [(1R,2R,3R,11S,12S,14R,26R)-5,12-dihydroxy-6,6'-dimethoxy-7,21,30-trimethyl-27-oxospiro[17,19,28-trioxa-24-thia-13,30-diazaheptacyclo[12.9.6.13,11.02,13.04,9.015,23.016,20]triaconta-4(9),5,7,15,20,22-hexaene-26,1'-2,3,4,9-tetrahydropyrido[3,4-b]indole]-22-yl] acetate
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC41H44N4O10S
Molar mass784.88 g·mol−1
3D model (JSmol)
  • CC1=CC2=C([C@@H]3[C@@H]4[C@H]5C6=C(C(=C7C(=C6[C@@H](N4[C@H]([C@H](C2)N3C)O)COC(=O)[C@@]8(CS5)C9=C(CCN8)C2=C(N9)C=CC(=C2)OC)OCO7)C)OC(=O)C)C(=C1OC)O
  • InChI=1S/C41H44N4O10S/c1-17-11-20-12-25-39(48)45-26-14-52-40(49)41(38-22(9-10-42-41)23-13-21(50-5)7-8-24(23)43-38)15-56-37(31(45)30(44(25)4)27(20)32(47)33(17)51-6)29-28(26)36-35(53-16-54-36)18(2)34(29)55-19(3)46/h7-8,11,13,25-26,30-31,37,39,42-43,47-48H,9-10,12,14-16H2,1-6H3/t25-,26-,30+,31+,37+,39-,41+/m0/s1
  • Key:YDDMIZRDDREKEP-HWTBNCOESA-N

Lurbinectedin, sold under the brand name Zepzelca, is a medication used for the treatment of small cell lung cancer.[5][6][7]

The most common side effects include leukopenia, lymphopenia, fatigue, anemia, neutropenia, increased creatinine, increased alanine aminotransferase, increased glucose, thrombocytopenia, nausea, decreased appetite, musculoskeletal pain, decreased albumin, constipation, dyspnea, decreased sodium, increased aspartate aminotransferase, vomiting, cough, decreased magnesium and diarrhea.[5][6][7]

Lurbinectedin is a synthetic tetrahydropyrrolo [4,3,2-de]quinolin-8(1H)-one alkaloid analogue with potential antineoplastic activity.[8] Lurbinectedin covalently binds to residues lying in the minor groove of DNA, which may result in delayed progression through S phase, cell cycle arrest in the G2/M phase and cell death.[8]

Lurbinectedin was approved for medical use in the United States in June 2020.[9][5][6][7][10]

  1. ^ a b "Zepzelca". Therapeutic Goods Administration (TGA). 22 September 2021. Archived from the original on 30 September 2021. Retrieved 30 September 2021.
  2. ^ a b "AusPAR: lurbinectedin". Therapeutic Goods Administration (TGA). 4 May 2022. Archived from the original on 4 May 2022. Retrieved 4 May 2022.
  3. ^ "Updates to the Prescribing Medicines in Pregnancy database". Therapeutic Goods Administration (TGA). 12 May 2022. Archived from the original on 3 April 2022. Retrieved 13 May 2022.
  4. ^ "Summary Basis of Decision (SBD) for Zepzelca". Health Canada. 23 October 2014. Archived from the original on 29 May 2022. Retrieved 29 May 2022.
  5. ^ a b c d "Zepzelca- lurbinectedin injection, powder, lyophilized, for solution". DailyMed. 15 June 2020. Archived from the original on 24 January 2021. Retrieved 24 September 2020.
  6. ^ a b c "Jazz Pharmaceuticals Announces U.S. FDA Accelerated Approval of Zepzelca (lurbinectedin) for the Treatment of Metastatic Small Cell Lung Cancer" (Press release). Jazz Pharmaceuticals. 15 June 2020. Archived from the original on 15 June 2020. Retrieved 15 June 2020 – via PR Newswire.
  7. ^ a b c "FDA grants accelerated approval to lurbinectedin for metastatic small". U.S. Food and Drug Administration (FDA). 15 June 2020. Archived from the original on 18 June 2020. Retrieved 16 June 2020. Public Domain This article incorporates text from this source, which is in the public domain.
  8. ^ a b "Lurbinectedin". National Cancer Institute. Archived from the original on 16 May 2020. Retrieved 15 June 2020. Public Domain This article incorporates text from this source, which is in the public domain.
  9. ^ "Zepzelca: FDA-Approved Drugs". U.S. Food and Drug Administration (FDA). Archived from the original on 19 October 2020. Retrieved 15 June 2020.
  10. ^ "Drug Trials Snapshots: Zepzelca". U.S. Food and Drug Administration (FDA). 15 June 2020. Archived from the original on 22 December 2020. Retrieved 28 June 2020. Public Domain This article incorporates text from this source, which is in the public domain.