Linker Information
General Information of This Linker
| Linker ID |
LIN0KDRVI
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| Linker Name |
Mal-PEG8-Val-Ala
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| Linker Type |
Cathepsin-cleavable linker
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| Antibody-Linker Relation |
Cleavable
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| Structure |
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| Formula |
C34H58N4O15
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| Isosmiles |
CC(NC(=O)C(NC(=O)CCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCN1C(=O)C=CC1=O)C(C)C)C(=O)O
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| InChI |
InChI=1S/C34H58N4O15/c1-26(2)32(33(43)36-27(3)34(44)45)37-29(40)7-10-46-12-14-48-16-18-50-20-22-52-24-25-53-23-21-51-19-17-49-15-13-47-11-8-35-28(39)6-9-38-30(41)4-5-31(38)42/h4-5,26-27,32H,6-25H2,1-3H3,(H,35,39)(H,36,43)(H,37,40)(H,44,45)
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| InChIKey |
GITGYODHQZKNBP-UHFFFAOYSA-N
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| Pharmaceutical Properties |
Molecule Weight
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762.851
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Polar area
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235.82
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Complexity
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762.3898672
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xlogp Value
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-1.3293
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Heavy Count
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53
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Rot Bonds
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35
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Hbond acc
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14
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Hbond Donor
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4
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Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
AZD5335 [Phase 1/2]
Identified from the Human Clinical Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Related Clinical Trial | |||||
| NCT Number | NCT05797168 | Clinical Status | Phase 1/2 | ||
| Clinical Description |
FONTANA: A modular phase 1/2a, open-label, multi-center study to assess the safety, tolerability, pharmacokinetics, and preliminary efficacy of ascending doses of AZD5335 monotherapy and in combination with anti-cancer agents in participants with solid tumors.
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| Primary Endpoint |
Number of participants with adverse events/serious adverse events, the number of participants with dose limiting toxicity (DLT).
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| Other Endpoint |
Objective Response Rate (ORR), Duration of Response (DoR), Disease Control Rate (DCR), Progression free Survival (PFS), Overall Survival (OS).
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AZD8205 [Phase 1/2]
Identified from the Human Clinical Data
| Experiment 1 Reporting the Activity Date of This ADC | [2] | ||||
| 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 | Clinical 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 | [3] | ||||
| 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 | [4] | ||||
| 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 | Clinical 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