Lurbinectedin

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Cat Number

API497871473

CAS Number

497871-47-3

For research use only. We do not supply to patients.

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CAS Number

497871-47-3

Storage

Store at 2-8℃

Synonyms

PM01183; Tryptamicidin; Zepzelca; [(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

Molecular Formula

C41H44N4O10S

Molecular Weight

784.9

Smiles

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

General Description

Lurbinectedin, also known as PM01183, is a synthetic analogue of trabectedin. It is a pentacyclic compound with two fused tetrahydroisoquinoline rings and a tetrahydro β-carboline recognition unit. It binds to the minor groove of DNA and associates with the hydroxyl of its hemiaminal group to the central guanine of CGG, AGC, AGG and TGG DNA triplets.

Mechanism of Action

Lurbinectedin forms covalent adducts with guanine residues in the minor groove of DNA. These adducts can result in double-strand DNA breaks, as well as interfere with DNA-protein interactions and RNA transcription. Lurbinectedin specifically targets CG-rich DNA sequences found in the promoter regions of protein-coding genes. In addition to its effects on DNA, lurbinectedin contributes to its anti-tumor activity by inhibiting RNA transcription and inducing degradation of elongating RNA polymerase II.

Application

Lurbinectedin has antitumor activity with manageable AEs in patients with platinum-sensitive and platinum-resistant SCLCs and in patients with recurrent SCLCs who progressed after receiving second-line treatment and this agent has been FDA approved for patients with metastatic SCLCs who have disease progression on or after platinum-based chemotherapy. Lurbinectedin has also demonstrated activity against malignant pleural mesothelioma, sarcoma, in particular leiomyosarcoma, myxoid liposarcoma, and dedifferentiated liposarcoma, and ovarian and endometrial carcinoma.

By DNA binding, lurbinectedin traps and targets RNA Pol II to proteasomal degradation. This inhibits RNA synthesis and also leads to the formation of DNA breaks that are erroneously repaired by the TCR system. DNA breaks also cause S-phase cell cycle arrest and ultimately result in apoptosis. In SCLC-A and SCLC-N subtypes, lurbinectedin preferentially targets and blocks activated ASCL1- and NEUROD1-mediated transcriptional activity, downregulating several genes.

Fig. 1 Chemical structure and mechanism of action of lurbinectedin. (Calles A, et al. 2025)

References

Calles A, et al. Unveiling the mechanism of lurbinectedin’s action and its potential in combination therapies in small cell lung cancer. Molecular Cancer Therapeutics. 2025, 24(6): 828-839.

Novel functionalized graphene oxide (GO) nanoparticles (NPs) are a new generation of drug nanocarriers for potential targeted therapy in lung cancer. The biocompatible GO NPs were used as delivery vehicles for Quercetin (Qn) and Lurbinectedin (Ln) to show their synergistic anti-cancer effect in A549 and PC9 lung cancer cells. The physicochemical properties of GO NPs and their drug-loaded nanoformulation were confirmed by spectroscopic and microscopic techniques, as well as by the pH-dependent drug release behavior.
The Qn and Ln-loaded GO NPs induced a significantly higher cytotoxic effect than the free drugs, leading to apoptosis, evidenced by morphological changes, nuclear fragmentation (DAPI staining), and ROS increase. This apoptotic effect at the molecular level was confirmed by qRT-PCR and Western blot, showing the activation of the pro-apoptotic pathway through the upregulation of p53, Bax, and Caspase-3 and downregulation of Bcl-2. Finally, the scratch wound-healing assay also revealed the potential of this nanoformulation to suppress cell migration and metastasis. In conclusion, Qn/Ln-loaded GO NPs represent a novel targeted delivery system with potential improvement of therapeutic efficacy for the treatment of lung cancer, reducing the limitations of classical chemotherapy.

Fig. 2 Schematic representation of Qn/Ln-GO NPs and its applications. (Liao R, et al. 2024)

References

Liao R, et al. Functionalized graphene oxide NPs as a nanocarrier for drug delivery system in quercetin/lurbinectedin as dual sensitive therapeutics for A549 lung cancer treatment. Heliyon. 2024, 10(11).

Is Lurbinectedin sensitive to humidity in the storage environment?

Lurbinectedin is hygroscopic; it should be stored in a dry place with desiccants.

How can I request a price quote for Lurbinectedin?

Please submit an inquiry specifying the required quantity and purity of Lurbinectedin needed.

Can I modify my Lurbinectedin order after the invoice is paid?

Order modifications for Lurbinectedin are possible if requested before the final packaging stage.

Is a catch-specific certificate of analysis provided for every Lurbinectedin order?

Yes, every shipment of Lurbinectedin is accompanied by a detailed, batch-specific COA.