ADC Name	RG7598
Synonyms	RG7598; DFRF4539A; DFRF-4539A    Click to Show/Hide
Organization	Genentech (Top20 MNC) (Originator)
Drug Status	Phase 1 (discontinued)
Drug-to-Antibody Ratio	4
Structure
	3D MOL			2D MOL
Antibody Name	MFRF3266A					Antibody Info
Antigen Name	Fc receptor-like protein 5 (FCRL5)					Antigen Info
Payload Name	Monomethyl auristatin E					Payload Info
Payload Target	Microtubule (MT)					Target Info
Linker Name	Mc-Val-Cit-PABC					Linker Info
Conjugate Type	Random Cysteines
Combination Type	vedotin

Standard Type	Value	Units	Description	Reference
Maximum Observed Concentration (Cmax)	55.1	ug/mL	Mean (% CV) for DFRF4539A pharmacokinetic parameter analytes-in cycle 1 at 2.4 mg/kg.	[1]
Area Under the Concentration-Time Curve (AUC)	291	day·ug/mL	Mean (% CV) for DFRF4539A pharmacokinetic parameter analytes-in cycle 1 at 2.4 mg/kg, AUCinf.	[1]

Standard Type	Value	Units	Description	Reference
Clearance (CL)	9.6	mL/day/kg	Mean (% CV) for DFRF4539A pharmacokinetic parameter analytes-in cycle 1 at 2.4 mg/kg.	[1]

Standard Type	NCT Number	Clinical Status	Clinical Trial Description
Undisclosed	NCT01432353	PHASE1	An Open-label, Multicenter, Phase I Trial of the Safety and Pharmacokinetics of Escalating Doses of DFRF4539A in Patients With Relapsed or Refractory Multiple Myeloma

Experiment 1 Reporting the Activity Date of This ADC					[1]
Patients Enrolled	Eligibility requires adults (≥18) with ECOG 0-2, relapsed/refractory myeloma (prior proteasome inhibitor/immunomodulatory therapy), and measurable disease. Exclusions: recent mAb/chemotherapy (≤4/2 weeks), unresolved toxicities (except neuropathy), recent transplants, antibody allergies, active infections, or hepatitis/HIV. Pregnancy is prohibited.    Click to Show/Hide
Administration Dosage	multiple ascending doses
Related Clinical Trial
NCT Number	NCT01432353	Clinical Status	PHASE1
Clinical Description	An Open-label, Multicenter, Phase I Trial of the Safety and Pharmacokinetics of Escalating Doses of DFRF4539A in Patients With Relapsed or Refractory Multiple Myeloma
Primary Endpoint	The study evaluates safety outcomes including AE incidence over 3.5 years, MTD/DLT determination within 1.5 years, and establishes the RP2D for DFRF4539A administered every 3 weeks or weekly.
Other Endpoint	Immunogenicity (serum ATA levels) and PK (AUC) are monitored over 3.5 years. Efficacy is assessed via IMWG/EBMT criteria for objective response, DoR (time to progression/death), and PFS (from treatment initiation to progression/death within 30 days post-treatment).

Ref 1	Phase I study of the anti-FcRH5 antibody-drug conjugate DFRF4539A in relapsed or refractory multiple myeloma