Lurbinectedin (PM01183)

For research use only.

Catalog No.S9603 Synonyms: PM-1183, LY-01017, Tryptamicidin, Zepsyre, ZEPZELCA

Lurbinectedin (PM01183) Chemical Structure

CAS No. 497871-47-3

Lurbinectedin (PM01183, PM-1183, LY-01017, Tryptamicidin, Zepsyre, ZEPZELCA), a DNA minor groove covalent binder with potent in vitro and in vivo anti-tumour activity. Lurbinectedin inhibits RMG1 and RMG2 cell growth with IC50 of 1.25 nM and 1.16 nM, respectively.

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Biological Activity

Description Lurbinectedin (PM01183, PM-1183, LY-01017, Tryptamicidin, Zepsyre, ZEPZELCA), a DNA minor groove covalent binder with potent in vitro and in vivo anti-tumour activity. Lurbinectedin inhibits RMG1 and RMG2 cell growth with IC50 of 1.25 nM and 1.16 nM, respectively.
Targets
DNA minor groove [1]
()
RMG2 cell growth [1]
(Cell-based assay)
RMG1 cell growth [1]
(Cell-based assay)
1.16 nM 1.25 nM
In vitro

Lurbinectedin exhibits significant antitumor activity toward chemosensitive and chemoresistant CCC cells in vitro. Lurbinectedin plus SN-38 combination has strong synergistic effects on both the cisplatin-resistant and paclitaxel-resistant CCC cell lines.[1]

In vivo

An examination of mouse CCC cell xenografts reveals that lurbinectedin significantly inhibits tumor growth. Lurbinectedin plus SN-38 combination results in a significant synergistic effect. Everolimus significantly enhances the antitumor activity of lurbinectedin-based chemotherapies.[1]

Protocol

Cell Research:

[1]

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  • Cell lines: The human ovarian CCC cell lines (RMG1, RMG2, KOC7C, HAC2)
  • Concentrations: 0.1 nM, 0.3 nM, 1 nM, 3 nM
  • Incubation Time: 48 h
  • Method:

    CCC cells (2~5×105) are treated with lurbinectedin, SN38 or in combination of the two drugs at the indicated concentrations for 48 hours. Then, the cells are harvested and stained with PI and annexin V using the annexin V-fluorescein isothiocyanate (FITC) apoptosis detection kit, according to the manufacturer's instructions. Fluorescence data are collected using flow cytometry. The sum total of early apoptotic cells (annexin V(+), PI(−) cells) and late apoptotic cells (annexin V(+), PI(+) cells) is defined as the total number of apoptotic cells. The experiments are repeated at least three times.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: 5- to 7-week-old nude mice
  • Dosages: 0.180 mg/kg
  • Administration: IV
    (Only for Reference)

Solubility (25°C)

Chemical Information

Molecular Weight 784.87
Formula

C41H44N4O10S

CAS No. 497871-47-3
Storage powder
in solvent
Synonyms PM-1183, LY-01017, Tryptamicidin, Zepsyre, ZEPZELCA
Smiles CC1=CC2=C(C3C4C5C6=C(C(=C7C(=C6C(N4C(C(C2)N3C)O)COC(=O)C8(CS5)C9=C(CCN8)C2=C(N9)C=CC(=C2)OC)OCO7)C)OC(=O)C)C(=C1OC)O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04802174 Recruiting Drug: Lurbinectedin|Drug: Berzosertib SCLC|Small Cell Cancer|Advanced Solid Tumor|High Grade Neuroendocrine Cancers National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) June 1 2021 Phase 1|Phase 2
NCT04894591 Recruiting Drug: Zepzelca Extensive-stage Small-cell Lung Cancer Jazz Pharmaceuticals June 28 2021 --
NCT04610658 Recruiting Drug: Nivolumab|Drug: Ipilimumab|Drug: Lurbinectedin Small-cell Lung Cancer|Relapsed Small Cell Lung Cancer|Recurrent Small Cell Lung Cancer H. Lee Moffitt Cancer Center and Research Institute|Bristol-Myers Squibb|PharmaMar November 23 2020 Phase 1|Phase 2
NCT04358237 Recruiting Drug: Lurbinectedin|Drug: Pembrolizumab Small Cell Lung Carcinoma Antonio Calles Blanco|MedSIR|PharmaMar|Merck Sharp & Dohme Corp.|Blanco Dr Antonio Calles MD September 21 2020 Phase 1|Phase 2
NCT04253145 Recruiting Drug: PM 01183|Drug: Atezolizumab Carcinoma Small Cell Lung Fundacion Oncosur December 13 2019 Phase 1
NCT02451007 Completed Drug: lurbinectedin (PM01183) Solid Tumors PharmaMar August 12 2015 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID