Antibody Information

General Information of This Antibody (ID: ANTI0XVCLH)
Antibody Name
LMJ729
Antigen Name
c-Kit
  Antigen Info 
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Each Antibody-drug Conjugate Related to This Antibody
Full Information of The Activity Data of The ADC(s) Related to This Antibody
LOP628 [Phase 1 (discontinued)]
 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 [1]
Patients Enrolled
Eligibility criteria require documented cKit-positive neoplasms (solid tumors) or AML with specific progression patterns, measurable disease, and blast count limits (AML). Exclusion criteria address CNS metastases, significant comorbidities, prior cKit-directed antibody therapy, pregnancy, and prior bone marrow transplant (AML), ensuring patient safety while maintaining study validity across both tumor types.

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Administration Dosage
Infusions were given of either 0.3 mg/kg LOP628, without premedication, or 0.15 mg/kg LOP628, with premedication of dexamethasone and cetirizine.
Related Clinical Trial
NCT Number NCT02221505  Clinical Status PHASE1
Clinical Description
A Phase I, Multicenter, Open-label Dose Escalation and Expansion Study of LOP628, Administered Intravenously in Adult Patients With cKit-positive Tumors and Acute Myeloid Leukemia
Primary Endpoint
The study assesses the incidence of dose-limiting toxicities (DLTs) over 12 months to determine the maximum tolerated dose/recommended dose for expansion (MTD/RDE) of LOP628, evaluating its safety and feasibility at different dosage levels.
Other Endpoint
The trial evaluates multiple safety and efficacy endpoints over 30 months, including adverse event incidence, pharmacokinetics (PK) profiles (AUC, Cmax, etc.), and preliminary anti-tumor activity metrics (ORR, DOR, PFS, DCR, BOR). For AML patients, additional assessments like event-free survival (EFS) and duration of response are included to comprehensively characterize LOP628's therapeutic potential across hematological and solid tumor indications.

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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 [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 43.30% Positive KIT expression (KIT+++/++)
Method Description
The in vivo antitumor activity of LOP-628 was evaluated in a c-KIT positive GIST430 xenograft model. Animals were administered a single i.v. injection of the vehicle, IgG-ADC, or LOP628, LMJ729, imatinib.
In Vivo Model KIT-expressing GIST430 xenograft model
In Vitro Model Gastrointestinal stromal tumor GIST430 cells CVCL_7040
Experiment 2 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 46% Positive KIT expression (KIT+++/++)
Method Description
The in vivo antitumor activity of LOP-628 was evaluated in a c-KIT positive NCI-H1048 SCLC xenograft model. Animals were administered a single i.v. injection of the vehicle, IgG-ADC, or LOP628; twice daily 80 mg/kg oral doses of imatinib or the combination of LOP628 with imatinib.
In Vivo Model KIT-expressing NCI-H1048 SCLC xenograft model
In Vitro Model Lung small cell carcinoma NCI-H1048 cells CVCL_1453
Experiment 3 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 75% Positive KIT expression (KIT+++/++)
Method Description
The in vivo antitumor activity of LOP-628 was evaluated in a c-KIT positive GIST430 xenograft model. Animals were administered a single i.v. injection of the vehicle, IgG-ADC, or LOP628, LMJ729, imatinib.
In Vivo Model KIT-expressing GIST430 xenograft model
In Vitro Model Gastrointestinal stromal tumor GIST430 cells CVCL_7040
Experiment 4 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 80.20% Positive KIT expression (KIT+++/++)
Method Description
The in vivo antitumor activity of LOP-628 was evaluated in a c-KIT positive GIST-T1 xenograft model. Animals were administered a single i.v. injection of the vehicle, IgG-ADC, or LOP628; twice daily 80 mg/kg oral doses of imatinib or the combination of LOP628 with imatinib.
In Vivo Model KIT-expressing GIST-T1 xenograft model
In Vitro Model Gastrointestinal stromal tumor GIST-T1 cells CVCL_4976
Experiment 5 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI)
82.20%
Positive KIT expression (KIT+++/++)
Method Description
The in vivo antitumor activity of LOP-628 was evaluated in a c-KIT positive GIST-T1 xenograft model. An efficacy study (single 0.625 mg/kg dose) in the GIST-T1 xenograft model in mice was performed.
In Vivo Model KIT-expressing GIST-T1 xenograft model
In Vitro Model Gastrointestinal stromal tumor GIST-T1 cells CVCL_4976
Experiment 6 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 87.30% Positive KIT expression (KIT+++/++)
Method Description
The in vivo antitumor activity of LOP-628 was evaluated in a c-KIT positive NCI-H1048 SCLC xenograft model. Animals were administered a single i.v. injection of the vehicle, IgG-ADC, or LOP628; twice daily 80 mg/kg oral doses of imatinib or the combination of LOP628 with imatinib.
In Vivo Model KIT-expressing NCI-H1048 SCLC xenograft model
In Vitro Model Lung small cell carcinoma NCI-H1048 cells CVCL_1453
Experiment 7 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 93.30% Positive KIT expression (KIT+++/++)
Method Description
The in vivo antitumor activity of LOP-628 was evaluated in a c-KIT positive NCI-H1048 SCLC xenograft model. Animals were administered a single i.v. injection of the vehicle, IgG-ADC, or LOP628; twice daily 80 mg/kg oral doses of imatinib or the combination of LOP628 with imatinib.
In Vivo Model KIT-expressing NCI-H1048 SCLC xenograft model
In Vitro Model Lung small cell carcinoma NCI-H1048 cells CVCL_1453
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximum Growth Inhibitory Concentration (GI50) < 0.5 nM Positive KIT expression (KIT+++/++)
Method Description
The inhibitory activity of LOP-628 against cancer cell growth was compared with LMJ729 against cancer cell growth in vitro.
In Vitro Model Gastrointestinal stromal tumor GIST-T1 cells CVCL_4976
Experiment 2 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximum Growth Inhibitory Concentration (GI50) < 1 nM Positive KIT expression (KIT+++/++)
Method Description
The inhibitory activity of LOP-628 against cancer cell growth was compared with LMJ729 against cancer cell growth in vitro.
In Vitro Model Lung small cell carcinoma NCI-H526 cells CVCL_1569
Experiment 3 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximum Growth Inhibitory Concentration (GI50) > 10 nM Negative KIT expression (KIT-)
Method Description
The inhibitory activity of LOP-628 against cancer cell growth was compared with LMJ729 against cancer cell growth in vitro.
In Vitro Model Breast adenocarcinoma MDA-MB-468 cells CVCL_0419
References
Ref 1 Phase 1 Study of LOP628 in Adult Patients With cKit-positive Solid Tumors and Acute Myeloid Leukemia
Ref 2 Preclinical Antitumor Activity of a Novel Anti-c-KIT Antibody-Drug Conjugate against Mutant and Wild-type c-KIT-Positive Solid Tumors. Clin Cancer Res. 2018 Sep 1;24(17):4297-4308.