Payload Information

General Information of This Payload
Payload ID
PAY0QNUSP
Name
Maytansinoid
Synonyms
Maytansinoid; BP-23647
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Target(s) Microtubule (MT)
 Target Info 
Structure
Formula
C28H37ClN2O8
Isosmiles
C[C@H]1[C@H]2[C@@](O2)([C@H](CC(=O)N(C3=C(C(=CC(=C3)C/C(=C/C=C/[C@H](C4(CC1OC(=O)N4)O)OC)/C)OC)Cl)C)O)C
PubChem CID
126961960
InChI
InChI=1S/C28H37ClN2O8/c1-15-8-7-9-22(37-6)28(35)14-20(38-26(34)30-28)16(2)25-27(3,39-25)21(32)13-23(33)31(4)18-11-17(10-15)12-19(36-5)24(18)29/h7-9,11-12,16,20-22,25,32,35H,10,13-14H2,1-6H3,(H,30,34)/b9-7+,15-8+/t16-,20?,21+,22-,25+,27+,28?/m1/s1
InChIKey
QWPXBEHQFHACTK-ZHGMIJKISA-N
IUPAC Name
(2R,3S,5S,6S,16E,18E,20R)-11-chloro-6,21-dihydroxy-12,20-dimethoxy-2,5,9,16-tetramethyl-4,24-dioxa-9,22-diazatetracyclo[19.3.1.110,14.03,5]hexacosa-10,12,14(26),16,18-pentaene-8,23-dione
Pharmaceutical Properties
Molecule Weight
565.1
Polar area
130
Complexity
993
xlogp Value
1.5
Heavy Count
39
Rot Bonds
2
Hbond acc
8
Hbond Donor
3
The activity data of This Payload
Standard Type Value Units Cell line Disease Model Cell line ID Reference
Half Maximal Inhibitory Concentration (IC50) 0.167 nM
OVCAR-3 cells
Ovarian serous adenocarcinoma
CVCL_0465 
[1]
Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
TRPH-222 [Phase 1]
 ADC Info 
Identified from the Human Clinical Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Objective Response Rate (ORR)
22.70% (all)
Patients Enrolled
Patients with diffuse large B-cell lymphoma (DLBCL), follicular lymphoma (FL), mantle cell lymphoma (MCL), and marginal zone lymphoma (MZL) were enrolled. Patients had received a median of 4 prior systemic therapy.
Administration Dosage
TRPH-222 was administered IV 0.60 to 5.60 mg/kg once every 3 weeks.
Related Clinical Trial
NCT Number NCT03682796  Phase Status Phase 1
Clinical Description
Phase 1, multicenter, open-label study of the antibody-drug conjugate TRPH-222 in subjects with relapsed and/or refractory B-cell lymphoma.
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 7 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 51.00% (Day 28) Positive CD22 expression (CD22+++/++)
Method Description
In WSU-DLCL2 xenografts once weekly intravenous (IV) dosing with 1 mg/kg TRPH-222.
In Vivo Model Non-Hodgkin's lymphoma CDX model
In Vitro Model Diffuse large B-cell lymphoma WSU-DLCL2 cells CVCL_1902
Experiment 2 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 87.00% (Day 28) Positive CD22 expression (CD22+++/++)
Method Description
In Granta-519 xenografts,trph-222 was dosed at 10 mg/kg once weekly intravenous (IV).
In Vivo Model Mantle cell lymphoma CDX model
In Vitro Model Mantle cell lymphoma Granta-519 cells CVCL_1818
Experiment 3 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 91.00% (Day 28) Positive CD22 expression (CD22+++/++)
Method Description
In SU-DHL-2 xenografts,trph-222 was dosed at 10 mg/kg once weekly intravenous (IV).
In Vivo Model Diffuse large B cell lymphoma CDX model
In Vitro Model Diffuse large B-cell lymphoma SU-DHL-2 cells CVCL_9550
Experiment 4 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 28) Positive CD22 expression (CD22+++/++)
Method Description
In SU-DHL-4 xenografts,trph-222 was dosed at 10 mg/kg once weekly intravenous (IV).
In Vivo Model Diffuse large B cell lymphoma CDX model
In Vitro Model Diffuse large B-cell lymphoma SU-DHL-4 cells CVCL_0539
Experiment 5 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 28) Positive CD22 expression (CD22+++/++)
Method Description
In WSU-DLCL2 xenografts once every three-week intravenous (IV) dosing with 10 mg/kg TRPH-222.
In Vivo Model Non-Hodgkin's lymphoma CDX model
In Vitro Model Diffuse large B-cell lymphoma WSU-DLCL2 cells CVCL_1902
Experiment 6 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 28) Positive CD22 expression (CD22+++/++)
Method Description
In WSU-DLCL2 xenografts once weekly intravenous (IV) dosing with 10 mg/kg TRPH-222.
In Vivo Model Non-Hodgkin's lymphoma CDX model
In Vitro Model Diffuse large B-cell lymphoma WSU-DLCL2 cells CVCL_1902
Experiment 7 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 28) Positive CD22 expression (CD22+++/++)
Method Description
In WSU-DLCL2 xenografts once weekly intravenous (IV) dosing with 3 mg/kg TRPH-222.
In Vivo Model Non-Hodgkin's lymphoma CDX model
In Vitro Model Diffuse large B-cell lymphoma WSU-DLCL2 cells CVCL_1902
References
Ref 1 Antibody drug conjugates of cleavable amino-benzoyl-maytansinoids. Bioorg Med Chem. 2020 Dec 1;28(23):115785.
Ref 2 First-in-Human Phase I Study of ABBV-085, an Antibody-Drug Conjugate Targeting LRRC15, in Sarcomas and Other Advanced Solid Tumors. Clin Cancer Res. 2021 Jul 1;27(13):3556-3566. doi: 10.1158/1078-0432.CCR-20-4513.
Ref 3 Trph-222, a Novel Anti-CD22 Antibody Drug Conjugate (ADC), Has Signficant Anti-Tumor Activity in NHL Xenografts and Is Well Tolerated in Non-Human Primates. Blood. 2017 Dec 8;130 (Suppl_1) : 4105.
Ref 4 TRPH-222, a novel anti-CD22 antibody drug conjugate (ADC), has significant anti-tumor activity in NHL xenografts and reduces B cells in monkeys.

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