General Information of This Linker
Linker ID
LIN0NFAFY
Linker Name
Gly-Mal-Gly-Gly-Phe-Gly
Antibody-Linker Relation
Cleavable
Structure
Formula
C24H28N6O10
Isosmiles
O=C(O)CNC[C@@H](C(=O)NCC(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O)N1C(=O)C=CC1=O
InChI
InChI=1S/C24H28N6O10/c31-17(10-27-24(40)16(9-25-12-21(35)36)30-19(33)6-7-20(30)34)26-11-18(32)29-15(23(39)28-13-22(37)38)8-14-4-2-1-3-5-14/h1-7,15-16,25H,8-13H2,(H,26,31)(H,27,40)(H,28,39)(H,29,32)(H,35,36)(H,37,38)/t15-,16-/m0/s1
InChIKey
LYEUNXNIQUMXBE-HOTGVXAUSA-N
Pharmaceutical Properties
Molecule Weight
560.52
Polar area
240.41
Complexity
560.1866911
xlogp Value
-3.8851
Heavy Count
40
Rot Bonds
16
Hbond acc
9
Hbond Donor
7
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
BL-B01D1 [Phase 3]
Identified from the Human Clinical Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Objective Response Rate (ORR)
61.80% (NSCLC EGFR mutation)
40.50% (NSCLC EGFR wildtype)
14.30% (SCLC)
45.80% (NPC)
7.70% (HNSCC)
Patients Enrolled
Patients with locally advanced or metastatic solid tumors.
Administration Dosage
BL-B01D1 was administered intravenously at doses of 2.50, 3.00 mg/kg D1D8 Q3W and 4.50, 5.00, 6.00 mg/kg D1 Q3W.
Related Clinical Trial
NCT Number NCT05194982  Clinical Status Phase 1
Clinical Description
A phase 1 clinical study to evaluate the safety, tolerability, pharmacokinetic characteristics and preliminary efficacy of BL-B01D1 in patients with locally advanced or metastatic solid tumor.
Experiment 2 Reporting the Activity Date of This ADC [2]
Related Clinical Trial
NCT Number NCT05785039  Clinical Status Phase 2
Clinical Description
Phase 2a/2b clinical study to evaluate the safety, tolerability, pharmacokinetics and efficacy of BL-B01D1 for injection in patients with multiple solid tumors such as locally advanced or metastatic urinary system tumors.
Experiment 3 Reporting the Activity Date of This ADC [3]
Related Clinical Trial
NCT Number NCT05470348  Clinical Status Phase 1
Clinical Description
A phase 1 clinical study to evaluate the safety, tolerability, pharmacokinetic characteristics and preliminary efficacy of BL-B01D1 in patients with unresectable locally advanced or metastatic breast cancer and other solid tumors.
Experiment 4 Reporting the Activity Date of This ADC [4]
Related Clinical Trial
NCT Number NCT05393427  Clinical Status Phase 1
Clinical Description
A phase 1 clinical study to evaluate the safety, tolerability, pharmacokinetic characteristics and preliminary efficacy of BL-B01D1 in patients with locally advanced or metastatic urological tumors and other solid tumors.
Experiment 5 Reporting the Activity Date of This ADC [5]
Related Clinical Trial
NCT Number NCT05262491  Clinical Status Phase 1
Clinical Description
A phase 1 clinical study to evaluate the safety, tolerability, pharmacokinetic characteristics and preliminary efficacy of BL-B01D1 in patients with locally advanced or metastatic gastrointestinal tumor and other solid tumor.
References
Ref 1 BL-B01D1, a first-in-class EGFRxHER3 bispecific antibody-drug conjugate (ADC), in patients with locally advanced or metastatic solid tumor: Results from a first-in-human phase 1 study. J Clin Oncol. 2023 41:16_suppl, 3001-3001.
Ref 2 Phase IIa/IIb Clinical Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Efficacy of BL-B01D1 for Injection in Patients With Multiple Solid Tumors Such as Locally Advanced or Metastatic Urinary System Tumors, NCT05785039
Ref 3 A Phase I Clinical Study to Evaluate the Safety, Tolerability, Pharmacokinetic Characteristics and Preliminary Efficacy of BL-B01D1 in Patients With Unresectable Locally Advanced or Metastatic Breast Cancer and Other Solid Tumors, NCT05470348
Ref 4 A Phase I Clinical Study to Evaluate the Safety, Tolerability, Pharmacokinetic Characteristics and Preliminary Efficacy of BL-B01D1 in Patients With Locally Advanced or Metastatic Urological Tumors and Other Solid Tumors, NCT05393427
Ref 5 A Phase I Clinical Study to Evaluate the Safety, Tolerability, Pharmacokinetic Characteristics and Preliminary Efficacy of BL-B01D1 in Patients With Locally Advanced or Metastatic Gastrointestinal Tumor and Other Solid Tumor, NCT05262491