General Information of This Payload
Payload ID
PAY0HANQZ
Name
Camptothecin analogue ED04
Synonyms
Camptothecin analogue ED04
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Target(s) DNA topoisomerase 1 (TOP1)
Structure
Formula
C28H29FN4O6
Isosmiles
CC[C@@]1(O)C(=O)OCc2c1cc1n(c2=O)Cc2c-1nc1cc(F)c(C)c3c1c2[C@@H](NC(=O)[C@H](C)OCN)CC3
InChI
InChI=1S/C28H29FN4O6/c1-4-28(37)17-7-21-24-15(9-33(21)26(35)16(17)10-38-27(28)36)23-19(32-25(34)13(3)39-11-30)6-5-14-12(2)18(29)8-20(31-24)22(14)23/h7-8,13,19,37H,4-6,9-11,30H2,1-3H3,(H,32,34)/t13-,19-,28-/m0/s1
InChIKey
AWGWTUBRWCBFRS-ULMCSZMWSA-N
Pharmaceutical Properties
Molecule Weight
536.56
Polar area
145.77
Complexity
536.2071129
xlogp Value
1.95192
Heavy Count
39
Rot Bonds
5
Hbond acc
9
Hbond Donor
3
Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
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  Phase 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  Phase 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 [5]
Related Clinical Trial
NCT Number NCT05470348  Phase 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 [6]
Related Clinical Trial
NCT Number NCT05393427  Phase 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 [7]
Related Clinical Trial
NCT Number NCT05262491  Phase 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.
BL-M07D1 [Phase 3]
Identified from the Human Clinical Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [3]
Related Clinical Trial
NCT Number NCT05631964  Phase Status Phase 1
Clinical Description
A phase 1 clinical study to evaluate the safety, tolerability, pharmacokinetic characteristics, and initial efficacy of BL-M07D1 for injection in patients with locally advanced or metastatic digestive tract tumors and other solid tumors.
Experiment 2 Reporting the Activity Date of This ADC [4]
Patients Enrolled
Patients with locally advanced or metastatic HER2-positive/low-expression breast cancer and other solid tumors.
Related Clinical Trial
NCT Number NCT05461768  Phase Status Phase 1
Clinical Description
A phase 1 clinical study to evaluate the safety, tolerability, pharmacokinetic characteristics, and preliminary efficacy of BL-M07D1 injection in patients with locally advanced or metastatic HER2-positive/low-expression breast cancer and other solid tumors.
BL-M02D1 [Phase 1/2]
Identified from the Human Clinical Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [8]
Related Clinical Trial
NCT Number NCT05385692  Phase Status Phase 1
Clinical Description
Phase 1 clinical study to evaluate the safety, tolerability, pharmacokinetic characteristics and preliminary efficacy of injectable BL-M02D1 in patients with locally advanced or metastatic gastrointestinal tumors or other solid tumors.
Experiment 2 Reporting the Activity Date of This ADC [9]
Related Clinical Trial
NCT Number NCT05339685  Phase Status Phase 1
Clinical Description
Phase 1 clinical study to evaluate the safety, tolerability, pharmacokinetic characteristics and preliminary efficacy of injectable BL-M02D1 in patients with locally advanced or metastatic triple negative breast cancer or other solid tumors.
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 Initial Efficacy of BL-M07D1 for Injection in Patients With Locally Advanced or Metastatic Digestive Tract Tumors and Other Solid Tumors, NCT05631964
Ref 4 A Phase I Clinical Study to Evaluate the Safety, Tolerability, Pharmacokinetic Characteristics, and Preliminary Efficacy of BL-M07D1injection in Patients With Locally Advanced or Metastatic HER2-positive/Low-expression Breast Cancer and Other Solid Tumors, NCT05461768
Ref 5 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 6 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 7 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
Ref 8 Phase I Clinical Study to Evaluate the Safety, Tolerability, Pharmacokinetic Characteristics and Preliminary Efficacy of Injectable BL-M02D1 in Patients With Locally Advanced or Metastatic Gastrointestinal Tumors or Other Solid Tumors, NCT05385692
Ref 9 Phase I Clinical Study to Evaluate the Safety, Tolerability, Pharmacokinetic Characteristics and Preliminary Efficacy of Injectable BL-M02D1 in Patients With Locally Advanced or Metastatic Triple Negative Breast Cancer or Other Solid Tumors, NCT05339685