Payload Information
General Information of This Payload
| Payload ID | PAY0SBXIV |
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|---|---|---|---|---|---|---|
| Name | Maytansine derivative M24 |
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| Synonyms |
M24; HY-115928; CS-0433790
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| Target | Microtubule (MT) | |||||
| Structure |
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| Formula | C44H40Cl3N5O11S |
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| Isosmiles | CC1=CC(=CC(=C1Cl)C)OCCOC2=CC=C(C=C2)CN3CC(=O)N(C3=O)CC(=O)NC(CC4=CC=C(C=C4)OCC5=CC=C(C=C5)Cl)C(=O)NS(=O)(=O)C6=CC(=C(C=C6)Cl)[N+](=O)[O-] |
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| PubChem CID | ||||||
| InChI |
InChI=1S/C44H40Cl3N5O11S/c1-27-19-35(20-28(2)42(27)47)62-18-17-61-33-13-7-30(8-14-33)23-50-25-41(54)51(44(50)56)24-40(53)48-38(43(55)49-64(59,60)36-15-16-37(46)39(22-36)52(57)58)21-29-5-11-34(12-6-29)63-26-31-3-9-32(45)10-4-31/h3-16,19-20,22,38H,17-18,21,23-26H2,1-2H3,(H,48,53)(H,49,55)
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| InChIKey |
BBCRCNRTBDZUKL-UHFFFAOYSA-N
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| IUPAC Name |
2-[[2-[3-[[4-[2-(4-chloro-3,5-dimethylphenoxy)ethoxy]phenyl]methyl]-2,5-dioxoimidazolidin-1-yl]acetyl]amino]-N-(4-chloro-3-nitrophenyl)sulfonyl-3-[4-[(4-chlorophenyl)methoxy]phenyl]propanamide
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| Pharmaceutical Properties | Molecule Weight |
953.2 |
Polar area |
215 |
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Complexity |
1690 |
xlogp Value |
8.2 |
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Heavy Count |
64 |
Rot Bonds |
18 |
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Hbond acc |
11 |
Hbond Donor |
2 |
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Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
REGN5093-M114 [Phase 1 (discontinued)]
Identified from the Human Clinical Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Patients Enrolled |
Eligible: Advanced NSCLC (no standard options), ECOG 0-1, MET overexpression (fresh/archival biopsy ≤6 months old), measurable lesion (s) (expansion), adequate organ function. Excluded: Recent systemic therapy (<2 weeks/5 half-lives), unresolved toxicities (>grade 1), active CNS disease, uncontrolled infections (HIV/HBV/HCV), or concurrent malignancy. Prior irradiation requires documented progression in irradiated lesions.
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| Administration Dosage |
Cohorts A and B: REGN5093-M114 monotherapy. Cohort C: REGN5093-M114+cemiplimab combination.
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| Related Clinical Trial | |||||
| NCT Number | NCT04982224 | Phase Status | PHASE1|||PHASE2 | ||
| Clinical Description |
A Phase 1/2 Study of REGN5093-M114 (METxMET Antibody-Drug Conjugate) in Patients With MET Overexpressing Advanced Cancer
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| Primary Endpoint |
Phase 1 dose escalation will assess safety through DLTs (28-day window), TEAEs, SAEs, treatment discontinuations, deaths, and CTCAE grade 3+ lab abnormalities over ~2 years. Pharmacokinetics include serum concentrations of REGN5093-M114 (total/conjugated), plasma M24 levels, and cemiplimab concentrations (Cohort C). Phase 2 expands ORR evaluation.
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| Other Endpoint |
Efficacy/Safety (both phases): ORR, TEAEs, SAEs, treatment-limiting toxicities, lab abnormalities, PK of REGN5093-M114/M24/cemiplimab (Cohort C), and ADA incidence/titer against cemiplimab/REGN5093-M114. Tumor response endpoints (DOR, DCR, TTR, PFS, OS) are tracked over 2 years.
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References