Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ID: DRG0JJEUT)
| ADC Name |
Aprutumab ixadotin
|
|||||
|---|---|---|---|---|---|---|
| Synonyms |
aprutumab ixadotin; BAY1187982; BAY 1187982
Click to Show/Hide
|
|||||
| Organization |
Bayer (Top20 MNC) (Originator)
|
|||||
| Drug Status |
Phase 1 (discontinued)
|
|||||
| Drug-to-Antibody Ratio |
4 (1.7~5.1)
|
|||||
| Structure |
|
|||||
| Antibody Name |
Aprutumab
|
Antibody Info | ||||
| Antigen Name |
Fibroblast growth factor receptor 2 (FGFR2)
|
Antigen Info | ||||
| Payload Name |
Auristatin W
|
Payload Info | ||||
| Payload Target |
Microtubule (MT)
|
Target Info | ||||
| Linker Name |
Caproyl acid
|
Linker Info | ||||
| Conjugate Type |
Random Lysines
|
|||||
| Combination Type |
ixadotin
|
|||||
2027 Update
The disease landscape of This ADC
2027 Update
The clinical trial pipelines of This ADC
General Information of The Activity Data Related to This ADC
Identified from the Human Clinical Data
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 |
Eligibility requires age ≥18, ECOG 0-1, advanced FGFR2+ solid tumors refractory to standard therapy (MTD expansion limited to triple-negative breast cancer ≤4 prior lines). Exclusion covers hypersensitivity to monoclonal antibodies, recent (<4 weeks) anticancer therapy, unresolved treatment-related toxicity, active brain metastases, significant cardiac disease, coagulation disorders, and pregnancy/breastfeeding.
Click to Show/Hide
|
||||
| Administration Dosage |
A dose of 0.1 mg BAY 1187982 per kilogram (kg) body weight (BW) was chosen as the starting dose based on toxicology data. The investigational drug will be administered as a 1-hour IV infusion once every 21 days at the trial site (Day 1 of each 21-day Cycle). The maximum possible dose escalation will be 2-fold and not more than 0.5 mg/kg BW until maximum tolerated dose is selected
Click to Show/Hide
|
||||
| Related Clinical Trial | |||||
| NCT Number | NCT02368951 | Clinical Status | PHASE1 | ||
| Clinical Description | An Open-label,Phase I, Dose-escalation Trial to Evaluate the Safety, Tolerability, Maximum Tolerated Dose, Pharmacokinetic, and Pharmacodynamics of the Anti-FGFR2 Antibody Drug Conjugate BAY1187982 in Subjects With Advanced Solid Tumors Known to Express FGFR2. | ||||
| Primary Endpoint |
The trial focuses on identifying the maximum tolerated dose (MTD) of the investigational drug, defined as the highest dose with <20% dose-limiting toxicities (DLTs) during Cycle 1. Safety and tolerability endpoints include adverse events (AEs) and serious adverse events (SAEs) monitored for up to 2 years.
|
||||
| Other Endpoint |
Pharmacokinetic (PK) assessments include single- and multiple-dose Cmax, AUC (0-tlast), AUC (0-504), and AUC (0-inf) over specified cycles (1, 3, 5, etc.). Biological markers FGFR2, CK18, and nucleosome levels in tumor/plasma are evaluated at screening and treatment milestones. Anti-drug antibodies (ADAs) and tumor response per RECIST are measured to assess immunogenicity and efficacy.
Click to Show/Hide
|
||||
| Experiment 2 Reporting the Activity Date of This ADC | [2] | ||||
| Patients Enrolled |
Advanced solid tumors from cancer indications known to be FGFR2-positive, which were refractory to any standard therapy or had no standard therapy available, patients were required to have measurable disease, Eastern Cooperative Oncology Group performance status (ECOG PS) of 0-1, an expected lifespan of at least 12 weeks.
|
||||
| Administration Dosage |
The starting dose was 0.1 mg/kg body weight, with doses increased in two-fold increments up to 0.80 mg/kg, after which the dose was escalated in 0.50 mg/kg increments, intravenously on day 1 of every 21-day cycle.
|
||||
| Related Clinical Trial | |||||
| NCT Number | NCT02368951 | Clinical Status | Phase 1 | ||
| Clinical Description | An open-label,phase 1, dose-escalation trial to evaluate the safety, tolerability, maximum tolerated dose, pharmacokinetic, and pharmacodynamics of the anti-FGFR2 antibody drug conjugate BAY1187982 in subjects with advanced solid tumors known to express FGFR2. | ||||
| Primary Endpoint |
Primary endpoints included safety, tolerability, and The MTD was determined to be 0.20 mg/kg.
|
||||
| Other Endpoint |
Secondary endpoints were pharmacokinetic evaluation and tumor response to aprutumab ixadotin.
|
||||
References