Payload Information
General Information of This Payload
| Payload ID | PAY0VZNCV |
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| Name | HDP 30.2115 |
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| Synonyms |
HDP 30.2115
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| Target | RNA polymerase II | |||||
| Structure |
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| Formula | C40H58N10O11S |
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| Isosmiles | CCC(C)C1NC(=O)CNCC2Cc3c([nH]c4ccccc34)SCC(NC(=O)CNCC1=O)C(=O)NC(CC(N)=O)C(=O)N1CC(O)CC1C(=O)NC(C(C)C(O)CO)C(=O)N2 |
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| InChI |
InChI=1S/C40H58N10O11S/c1-4-19(2)34-29(53)13-43-14-32(56)45-27-18-62-39-24(23-7-5-6-8-25(23)47-39)9-21(12-42-15-33(57)48-34)44-38(60)35(20(3)30(54)17-51)49-37(59)28-10-22(52)16-50(28)40(61)26(11-31(41)55)46-36(27)58/h5-8,19-22,26-28,30,34-35,42-43,47,51-52,54H,4,9-18H2,1-3H3,(H2,41,55)(H,44,60)(H,45,56)(H,46,58)(H,48,57)(H,49,59)
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| InChIKey |
JRGTXZHGUBMBQP-UHFFFAOYSA-N
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| Pharmaceutical Properties | Molecule Weight |
887.03 |
Polar area |
326.51 |
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Complexity |
62 |
xlogp Value |
-4.1254 |
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Heavy Count |
62 |
Rot Bonds |
7 |
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Hbond acc |
14 |
Hbond Donor |
12 |
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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
Pamlectabart tismanitin [Phase 1/2]
Identified from the Human Clinical Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Patients Enrolled |
Eligibility requires adults (≥18) with IMWG-defined active MM after ≥3 prior lines (IMiD/PI/anti-CD38) who are transplant-ineligible/post-SCT, excluding those with plasma cell leukemia, active CNS/other malignancies, uncontrolled infections (HIV/HBV/HCV), or recent SCT/radiotherapy (<12/<21 weeks). Phase 2a specifically excludes prior BCMA-targeted therapy exposure.
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| Administration Dosage |
Participants will receive HDP-101 intravenously in a 21 day cycle until disease progression, intolerable toxicity, Investigator's discretion or patient withdrawal.During the phase 1 tolerability of different dose levels will be evaluated. During the phase 2a dose expansion part the recommended phase 2 dose (RP2D) of HDP-101 will be administered.
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| Related Clinical Trial | |||||
| NCT Number | NCT04879043 | Phase Status | PHASE1|||PHASE2 | ||
| Clinical Description |
A Phase 1/2a, First-in-human Study to Evaluate the Safety, Tolerability, Pharmacokinetics, and Efficacy of HDP-101 in Patients With Plasma Cell Disorders Including Multiple Myeloma
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| Primary Endpoint |
Primary endpoints evaluate safety (dose-limiting toxicities during first 21-day cycle) and efficacy (objective response rate per IMWG criteria including sCR/CR/VGPR/PR) in relapsed/refractory multiple myeloma patients over approximately 1 year.
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| Other Endpoint |
Secondary objectives include comprehensive safety assessment (CTCAE v5.0 graded AEs) and clinical activity measures (PFS/OS) to characterize HDP-101's therapeutic profile, with all endpoints monitored throughout the 1-year study duration.
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Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.01 nM
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| Method Description |
The inhibitory activity of HDP-101 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 2 or 4 days.
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| In Vitro Model | Plasma cell myeloma | U266B1 cells | CVCL_0566 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.04 nM
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| Method Description |
The inhibitory activity of HDP-101 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 2 or 4 days.
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| In Vitro Model | Plasma cell myeloma | NCI-H929 cells | CVCL_1600 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.16 nM
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| Method Description |
The inhibitory activity of HDP-101 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 2 or 4 days.
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| In Vitro Model | Plasma cell myeloma | MM1.S cells | CVCL_8792 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.18 nM
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| Method Description |
The inhibitory activity of HDP-101 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 2 or 4 days.
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| In Vitro Model | Plasma cell myeloma | INA-6 cells | CVCL_5209 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.3 nM
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| Method Description |
The inhibitory activity of HDP-101 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 2 or 4 days.
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| In Vitro Model | Plasma cell myeloma | LP-1 cells | CVCL_0012 | ||
| Experiment 6 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.34 nM
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| Method Description |
The inhibitory activity of HDP-101 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 2 or 4 days.
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| In Vitro Model | Multiple myeloma | SK-MM-1 cells | CVCL_A478 | ||
| Experiment 7 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
4.83 nM
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| Method Description |
The inhibitory activity of HDP-101 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 2 or 4 days.
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| In Vitro Model | Plasma cell myeloma | L-363 cells | CVCL_1357 | ||
| Experiment 8 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
34.2 nM
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| Method Description |
The inhibitory activity of HDP-101 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 2 or 4 days.
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| In Vitro Model | Plasma cell myeloma | OPM-2 cells | CVCL_1625 | ||
| Experiment 9 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
142 nM
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| Method Description |
The inhibitory activity of HDP-101 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 2 or 4 days.
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| In Vitro Model | Plasma cell myeloma | RPMI-8226 cells | CVCL_0014 | ||
| Experiment 10 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | |||
| Method Description |
The inhibitory activity of HDP-101 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 2 or 4 days.
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| In Vitro Model | Osteosarcoma | U2OS cells | CVCL_0042 | ||
| Experiment 11 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 1000 nM | |||
| Method Description |
The inhibitory activity of HDP-101 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 2 or 4 days.
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| In Vitro Model | Normal | HS-5 cells | CVCL_3720 | ||
References