Payload Information
General Information of This Payload
| Payload ID | PAY0OWZGZ |
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|---|---|---|---|---|---|---|
| Name | AZ0132 |
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| Synonyms |
AZ0132
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| Target(s) | DNA topoisomerase 1 (TOP1) | |||||
| Structure |
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| Formula | C23H23N3O4 |
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| Isosmiles | CC[C@]1(O)C(=O)OCc2c1ccn(Cc1cnc3ccc(N)c4c3c1CCC4)c2=O |
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| InChI |
InChI=1S/C23H23N3O4/c1-2-23(29)17-8-9-26(21(27)16(17)12-30-22(23)28)11-13-10-25-19-7-6-18(24)15-5-3-4-14(13)20(15)19/h6-10,29H,2-5,11-12,24H2,1H3/t23-/m1/s1
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| InChIKey |
YYRXARNADRRMMV-HSZRJFAPSA-N
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| Pharmaceutical Properties | Molecule Weight |
405.454 |
Polar area |
107.44 |
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Complexity |
405.1688562 |
xlogp Value |
2.1701 |
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Heavy Count |
30 |
Rot Bonds |
3 |
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Hbond acc |
7 |
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
AZD8205 [Phase 1/2]
Identified from the Human Clinical Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Patients Enrolled |
Patients 18 years old with cholangiocarcinoma, breast, ovarian or endometrial cancers and ECOG PS 0-1.
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| Related Clinical Trial | |||||
| NCT Number | NCT05123482 | Phase Status | Phase 1/2 | ||
| Clinical Description |
A phase 1/2a multi-center, open-label master protocol to evaluate the safety, tolerability, pharmacokinetics, pharmacodynamics and preliminary antitumor activity of AZD8205 in participants with advanced or metastatic solid malignancies.
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Discovered Using Patient-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Objective Response Rate (ORR) |
69.00%
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Positive VTCN1 expression (VTCN1+++/++) | ||
| Method Description |
In the study of 26 PDX tumors,single administration of 3.5 mg/kg AZD8205 to determine the ORR,according to modified RECIST criteria,which correlated with homologous recombination repair (HRR) deficiency (HRD) and elevated levels of B7-H4 in HRR-proficient models.
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| In Vivo Model | Multiple tumor PDX model | ||||
AZD9592 [Phase 1]
Identified from the Human Clinical Data
| Experiment 1 Reporting the Activity Date of This ADC | [3] | ||||
| Patients Enrolled |
Patients with metastatic non-small cell lung cancer (mNSCLC) with EGFRm (sensitizing L858R mutation or exon 19 deletions) or EGFR wild-type, or recurrent or metastatic head and neck squamous cell carcinoma (HNSCC).
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| Related Clinical Trial | |||||
| NCT Number | NCT05647122 | Phase Status | Phase 1 | ||
| Clinical Description |
A phase 1, multicenter, open-label, first-in-human, dose escalation and expansion study of AZD9592 as monotherapy and in combination with anti-cancer agents in patients with advanced solid tumors.
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References