497871-47-3 Usage
Description
Lurbinectedin, a synthetic tetrahydropyrrolo[4,3,2-de]quinolin-8(1H)-one alkaloid analogue, is a potent antineoplastic agent with significant potential in the treatment of various cancers. It exerts its antineoplastic activity by covalently binding to DNA residues in the minor groove, leading to delayed progression through the S phase, cell cycle arrest in the G2/M phase, and ultimately, cell death. Lurbinectedin was approved for medical use in the United States in June 2020.
Uses
Used in Oncology:
Lurbinectedin is used as an antineoplastic agent for the treatment of various cancers, particularly metastatic small cell lung cancer (SCLC). It is indicated for adult patients with metastatic SCLC who have experienced disease progression on or after platinum-based chemotherapy. The drug's unique mechanism of action, which involves binding to DNA and disrupting cell cycle progression, makes it a valuable addition to the arsenal of cancer treatments.
Used in Drug Development:
Lurbinectedin serves as a promising candidate for further research and development in the field of oncology. Its approval for medical use in the United States has opened doors for additional studies to explore its potential in treating other types of cancer and improving the overall efficacy of cancer treatment regimens. As a result, Lurbinectedin may play a crucial role in the development of novel therapeutic strategies and drug delivery systems to enhance its bioavailability and therapeutic outcomes in various cancer applications.
Biological Activity
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.
Side effects
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.
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.
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.
Mode of action
Lurbinectedin is an Alkylating Drug. The mechanism of action of lurbinectedin is as an Alkylating Activity.
Check Digit Verification of cas no
The CAS Registry Mumber 497871-47-3 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 4,9,7,8,7 and 1 respectively; the second part has 2 digits, 4 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 497871-47:
(8*4)+(7*9)+(6*7)+(5*8)+(4*7)+(3*1)+(2*4)+(1*7)=223
223 % 10 = 3
So 497871-47-3 is a valid CAS Registry Number.
