Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0SNURI
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| ADC Name |
OBI-999
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| Synonyms |
OBI 999; OBI999; Globo H ADC
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| Organization |
OBI Pharma, Inc.
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| Drug Status |
Phase 1/2
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| Indication |
In total 1 Indication(s)
Solid tumors [ICD11:2A00-2A0Z|2B50-2F9Z]
Phase 2
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| Drug-to-Antibody Ratio |
4
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| Structure |
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| Antibody Name |
OBI-888
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Antibody Info | ||||
| Antigen Name |
Globo H (globotriaosylceramide)
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Antigen Info | ||||
| Payload Name |
Monomethyl auristatin E
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Payload Info | ||||
| Therapeutic Target |
Microtubule (MT)
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Target Info | ||||
| Linker Name |
ThioBridge-PEG24-Val-Ala-PAB
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Linker Info | ||||
| Conjugate Type |
Rebridge conjugation through reduced inter-chain cysteines.
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| Drugbank ID | ||||||
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General Information of The Activity Data Related to This ADC
Identified from the Human Clinical Data
Discovered Using Cell Line-derived Xenograft Model
Revealed Based on the Cell Line Data
| Standard Type | Value | Units | Cell Line | Disease Model |
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| Tumor Growth Inhibition value (TGI) |
≈ 70.7
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%
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MDA-MB-231 cells
HCC1428 cells |
Breast adenocarcinoma
Breast adenocarcinoma |
Full List of Activity Data of This Antibody-drug Conjugate
Identified from the Human Clinical Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Patients Enrolled |
Advanced solid tumors that had been previously treated with standard-of-care therapy and their physicians had determined that such therapy was no longer effective, or patients had declined to receive further standard-of-care treatments.
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| Administration Dosage |
The starting dose of 0.40 mg/kg on day 1 of each 21-day cycle; A standard 3 + 3 dose-escalation design was used, and doses of 0.80, 1.20, and 1.60 mg/kg were also administered on day 1 of each 21-day cycle; intravenous infusion over 60 minutes.
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| Related Clinical Trial | |||||
| NCT Number | NCT04084366 | Clinical Status | Phase 1 | ||
| Clinical Description | A phase 1/2, open-label, dose-escalation and cohort-expansion study evaluating the safety, pharmacokinetics, and therapeutic activity of OBI-999 in patients with advanced solid tumors. | ||||
| Primary Endpoint |
The incidence of dose-limiting toxicities and adverse events and determination of the maximum tolerated dose (MTD)/recommended phase II dose.
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Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 34.00% (Day 26) | Positive Globo H expression (Globo H+++/++) | ||
| Method Description |
Mice were treated with an intravenous dose of the ADCs at 0.3 mg/kg, qw*6.
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| In Vivo Model | MCF-7 CDX model | ||||
| In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 60.00% (Day 77) | Positive Globo H expression (Globo H+++/++) | ||
| Method Description |
Mice were treated with an intravenous dose of the ADCs at 1 mg/kg, qw*6.
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| In Vivo Model | MCF-7 CDX model | ||||
| In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 83.00% (Day 53) | Positive Globo H expression (Globo H+++/++) | ||
| Method Description |
Mice were treated with an intravenous dose of the ADCs at 1 mg/kg, qw*4.
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| In Vivo Model | NCI-N87 CDX model | ||||
| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 85.00% (Day 25) | Positive Globo H expression (Globo H+++/++) | ||
| Method Description |
Mice were treated with an intravenous dose of the ADCs at 10 mg/kg, qw*4.
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| In Vivo Model | NCI-H526 CDX model | ||||
| In Vitro Model | Lung small cell carcinoma | NCI-H526 cells | CVCL_1569 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 95.00% (Day 77) | Positive Globo H expression (Globo H+++/++) | ||
| Method Description |
Mice were treated with an intravenous dose of the ADCs at 10 mg/kg, qw*2.
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| In Vivo Model | MCF-7 CDX model | ||||
| In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
| Experiment 6 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 97.00% (Day 53) | Positive Globo H expression (Globo H+++/++) | ||
| Method Description |
Mice were treated with an intravenous dose of the ADCs at 10 mg/kg, qw*4.
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| In Vivo Model | NCI-N87 CDX model | ||||
| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
| Experiment 7 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 97.00% (Day 53) | Positive Globo H expression (Globo H+++/++) | ||
| Method Description |
Mice were treated with an intravenous dose of the ADCs at 1-3 mg/kg, qw*4.
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| In Vivo Model | NCI-N87 CDX model | ||||
| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
| Experiment 8 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 98.00% (Day 77) | Positive Globo H expression (Globo H+++/++) | ||
| Method Description |
Mice were treated with an intravenous dose of the ADCs at 3 mg/kg, qw*6.
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| In Vivo Model | MCF-7 CDX model | ||||
| In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
| Experiment 9 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 99.00% (Day 37) | Positive Globo H expression (Globo H+++/++) | ||
| Method Description |
Mice were treated with an intravenous dose of the ADCs at 10 mg/kg, qw*4.
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| In Vivo Model | HPAC CDX model | ||||
| In Vitro Model | Pancreatic adenocarcinoma | HPAC cells | CVCL_3517 | ||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 70.70% | |||
| Method Description |
In vivo , In each animal study,the antitumor efficacy was evaluated with doses of 1.00, 3.00, or 10.00 mg/kg of OBI-999 via i.v. injection. In NCI-N87 xenograft model,treatment groups of MMAE 0.191 mg/kg and Ctrl-ADC 3 mg/kg were also included. Each study utilized 6 to 8 mice per group.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells | CVCL_0062 | ||
| Breast adenocarcinoma | HCC1428 cells | CVCL_1252 | |||
References
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