Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0JJEUT
ADC Name	Aprutumab ixadotin
Synonyms	BAY-1187982; BAY1187982; FGFR2-ADC; BAY 1187982 Click to Show/Hide
Organization	Bayer AG
Drug Status	Phase 1
Indication	In total 1 Indication(s) Solid tumors [ICD11:2A00-2A0Z\|2B50-2F9Z] Phase 1
Drug-to-Antibody Ratio	4
Structure
	3D MOL	2D MOL
Antibody Name	Aprutumab		Antibody Info
Antigen Name	Fibroblast growth factor receptor 2 (FGFR2)		Antigen Info
Payload Name	Auristatin W derivative		Payload Info
Therapeutic Target	Microtubule (MT)		Target Info
Linker Name	N-5-carboxypentyl		Linker Info
Conjugate Type	Random conjugation through nucleophilic lysines.
Combination Type	BAY 1168650
Puchem SID	472422799 , 316908553 , 442064794 , 385749862 , 44069954
ChEBI ID	CHEMBL4650293

General Information of The Activity Data Related to This ADC

Identified from the Human Clinical Data

Click To Hide/Show 1 Activity Data Related to This Level

Standard Type	NCT Number	Clinical Status	Clinical Trial Description
Undisclosed	NCT02368951	Phase 1	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. Click to Show/Hide

Full List of Activity Data of This Antibody-drug Conjugate

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	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

Ref 1	First-in-Human Phase I Study of Aprutumab Ixadotin, a Fibroblast Growth Factor Receptor 2 Antibody-Drug Conjugate (BAY 1187982) in Patients with Advanced Cancer. Target Oncol. 2019 Oct;14(5):591-601.