Linker Information
General Information of This Linker
| Linker ID |
LIN0TUSQC
|
|||||
|---|---|---|---|---|---|---|
| Linker Name |
Hydrophilic linker of XMT-2056
|
|||||
| Linker Type |
Unclear
|
|||||
| Antibody-Linker Relation |
Cleavable
|
|||||
| Structure |
|
|||||
| Formula |
C65H112N12O35
|
|||||
| Isosmiles |
OC([C@@H](NC(CCOCCOCCNC(CC[C@@H](C(NCC(NCC(NCC(NCC(NCCOCCOCCOCCOCCOCCOCCOCCOCCC(N[C@H](C(NC[C@@H]([C@H]([C@@H]([C@@H](CO)O)O)O)O)=O)CCC(NC[C@@H]([C@H]([C@@H]([C@@H](CO)O)O)O)O)=O)=O)=O)=O)=O)=O)=O)NC(CN1C(C=CC1=O)=O)=O)=O)=O)C)=O
|
|||||
| PubChem CID | ||||||
| InChI |
InChI=1S/C65H112N12O35/c1-41(65(101)102)74-50(86)8-12-103-16-18-105-14-10-66-48(84)4-2-43(76-56(92)38-77-57(93)6-7-58(77)94)64(100)73-37-55(91)71-36-54(90)70-35-53(89)69-34-52(88)67-11-15-106-19-21-108-23-25-110-27-29-112-31-30-111-28-26-109-24-22-107-20-17-104-13-9-51(87)75-42(63(99)72-33-45(81)60(96)62(98)47(83)40-79)3-5-49(85)68-32-44(80)59(95)61(97)46(82)39-78/h6-7,41-47,59-62,78-83,95-98H,2-5,8-40H2,1H3,(H,66,84)(H,67,88)(H,68,85)(H,69,89)(H,70,90)(H,71,91)(H,72,99)(H,73,100)(H,74,86)(H,75,87)(H,76,92)(H,101,102)/t41-,42-,43-,44-,45-,46+,47+,59+,60+,61+,62+/m0/s1
|
|||||
| InChIKey |
KWWOMQCVHJOVFM-MKOXISCLSA-N
|
|||||
| Pharmaceutical Properties |
Molecule Weight
|
1621.66
|
Polar area
|
689.38
|
||
|
Complexity
|
2672.746141
|
xlogp Value
|
-14.2217
|
|||
|
Heavy Count
|
112
|
Rot Bonds
|
70
|
|||
|
Hbond acc
|
34
|
Hbond Donor
|
22
|
|||
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
XMT-2056 [Phase 1]
Identified from the Human Clinical Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Patients Enrolled |
Eligible participants have HER2-positive recurrent/metastatic solid tumors with progressive disease, ECOG 0-1, and measurable lesions (RECIST 1.1). Key exclusions: recent immunosuppressive therapy (>10mg/day prednisone), prior STING-targeting treatment, active malignancy within 2 years (except low-risk cases), or untreated CNS metastases (stable/treated cases allowed with criteria).
Click to Show/Hide
|
||||
| Administration Dosage |
XMT-2056 will be administered through a vein in your arm or port catheter (intravenously)
|
||||
| Related Clinical Trial | |||||
| NCT Number | NCT05514717 | Clinical Status | PHASE1 | ||
| Clinical Description |
A Phase 1, First-in-Human, Dose Escalation and Expansion, Multicenter Study of XMT-2056 in Participants With Advanced/Recurrent Solid Tumors That Express HER2
|
||||
| Primary Endpoint |
Safety and primary objectives focus on evaluating dose-limiting toxicities (DLTs), determining the maximum tolerated dose (MTD), and assessing adverse events over 15 months (Dose Escalation) and up to 3 years (Dose Expansion). The Objective Response Rate (ORR) is measured per RECIST 1.1 for confirmed responses.
|
||||
| Other Endpoint |
Secondary outcomes include ORR, duration of response (DOR), disease control rate (DCR), and comprehensive pharmacokinetic assessments (Tmax, Cmax, AUC, clearance, half-life, volume of distribution, Ctrough) over 3 years. Immunogenicity is evaluated by measuring antidrug/neutralizing antibodies (ADA/NAb).
|
||||