Payload Information
General Information of This Payload
| Payload ID | PAY0PBONE |
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| Name | Auristatin W |
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| Synonyms |
Auristatin W
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| Target(s) | Microtubule (MT) | |||||
| Structure |
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| Formula | C45H73N7O8 |
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| Isosmiles | CC[C@H](C)[C@@H]([C@@H](CC(=O)N1CCC[C@H]1[C@H](OC)[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCCCO1)OC)N(C)C(=O)[C@@H](NC(=O)[C@@H](NC)C(C)C)C(C)C |
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| InChI |
InChI=1S/C45H73N7O8/c1-12-29(6)40(50(9)45(57)39(28(4)5)49-43(55)38(46-8)27(2)3)36(58-10)25-37(53)51-21-17-20-35(51)41(59-11)30(7)42(54)48-34(44(56)52-22-15-16-23-60-52)24-31-26-47-33-19-14-13-18-32(31)33/h13-14,18-19,26-30,34-36,38-41,46-47H,12,15-17,20-25H2,1-11H3,(H,48,54)(H,49,55)/t29-,30+,34-,35-,36+,38-,39-,40-,41+/m0/s1
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| InChIKey |
LVAXOBQOMZKMEK-QUAKAHINSA-N
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| Pharmaceutical Properties | Molecule Weight |
840.12 |
Polar area |
174.64 |
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Complexity |
839.5520623 |
xlogp Value |
4.0543 |
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Heavy Count |
60 |
Rot Bonds |
21 |
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Hbond acc |
9 |
Hbond Donor |
4 |
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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
Aprutumab ixadotin [Phase 1 (Terminated)]
Identified from the Human Clinical Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Patients Enrolled |
Advanced solid tumors from cancer indications known to be FGFR2-positive, which were refractory to any standard therapy or had no standard therapy available, patients were required to have measurable disease, Eastern Cooperative Oncology Group performance status (ECOG PS) of 0-1, an expected lifespan of at least 12 weeks.
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| Administration Dosage |
The starting dose was 0.1 mg/kg body weight, with doses increased in two-fold increments up to 0.80 mg/kg, after which the dose was escalated in 0.50 mg/kg increments, intravenously on day 1 of every 21-day cycle.
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| Related Clinical Trial | |||||
| NCT Number | NCT02368951 | Phase Status | Phase 1 | ||
| Clinical Description |
An open-label,phase 1, dose-escalation trial to evaluate the safety, tolerability, maximum tolerated dose, pharmacokinetic, and pharmacodynamics of the anti-FGFR2 antibody drug conjugate BAY1187982 in subjects with advanced solid tumors known to express FGFR2.
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| Primary Endpoint |
Primary endpoints included safety, tolerability, and The MTD was determined to be 0.20 mg/kg.
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| Other Endpoint |
Secondary endpoints were pharmacokinetic evaluation and tumor response to aprutumab ixadotin.
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References