ADC Name	Samatatug zovodotin
Synonyms	ICON-2; XB002    Click to Show/Hide
Organization	Zymeworks (Originator) (No Rights);Exelixis;Iconic Therapeutics (No Rights)
Drug Status	Phase 1 (discontinued)
Drug-to-Antibody Ratio	3.3
Structure
				2D MOL
Antibody Name	Samatatug					Antibody Info
Antigen Name	Tissue factor (F3)					Antigen Info
Payload Name	ZD02044					Payload Info
Payload Target	Microtubule (MT)					Target Info
Linker Name	Mc-PEG3-Val-Cit					Linker Info
Conjugate Type	Random Cysteines
Combination Type	zovodotin

Standard Type	Value	Units	Description	Reference
Maximum Observed Concentration (Cmax)	68.1	ug/mL	Pharmacokinetic profile of anti-TF mAb 25A3 with zovodotin linker-payload (XB002), 25A3 3mg/kg.	[1]
Area Under the Concentration-Time Curve (AUC)	214	day·ug/mL	Pharmacokinetic profile of anti-TF mAb 25A3 with zovodotin linker-payload (XB002), 25A3 3mg/kg.	[1]
Maximum Observed Concentration (Cmax)	165	ug/mL	Pharmacokinetic profile of anti-TF mAb 25A3 with zovodotin linker-payload (XB002), 25A3 6mg/kg.	[1]
Area Under the Concentration-Time Curve (AUC)	511	day·ug/mL	Pharmacokinetic profile of anti-TF mAb 25A3 with zovodotin linker-payload (XB002), 25A3 6mg/kg.	[1]

Standard Type	Value	Units	Description	Reference
Elimination Half-Life (t1/2)	1.9	day	Pharmacokinetic profile of anti-TF mAb 25A3 with zovodotin linker-payload (XB002), 25A3 3mg/kg.	[1]
Elimination Half-Life (t1/2)	2.2	day	Pharmacokinetic profile of anti-TF mAb 25A3 with zovodotin linker-payload (XB002), 25A3 6mg/kg.	[1]

Standard Type	NCT Number	Clinical Status	Clinical Trial Description
Undisclosed	NCT04925284	PHASE1	A Dose-Escalation and Expansion Study of the Safety and Pharmacokinetics of XB002 as Single-Agent and Combination Therapy in Subjects With Inoperable Locally Advanced or Metastatic Solid Tumors

Experiment 1 Reporting the Activity Date of This ADC					[2]
Patients Enrolled	Inclusion Criteria: Adults with inoperable/metastatic solid tumors (specific histologies for each cohort) who exhausted standard therapies. Required: measurable disease (RECIST 1.1), ECOG 0-1, adequate organ function, archived/fresh tumor tissue (≤3 years old), and controlled AEs (CTCAE v5 ≤G1). Exclusion Criteria: Prior disqualifying therapies, untreated brain metastases (unless stable ≥4 weeks post-treatment), major surgery (within 4 weeks), QTcF >480 ms, pregnancy/lactation, hypersensitivity to study drugs, or active malignancies (except cured non-melanoma skin cancers/localized tumors).    Click to Show/Hide
Administration Dosage	Dose-escalation followed by cohort-expansion in tumor-specific expansion cohorts
Related Clinical Trial
NCT Number	NCT04925284	Clinical Status	PHASE1
Clinical Description	A Dose-Escalation and Expansion Study of the Safety and Pharmacokinetics of XB002 as Single-Agent and Combination Therapy in Subjects With Inoperable Locally Advanced or Metastatic Solid Tumors
Primary Endpoint	The study's Dose-Escalation Stage aimed to determine the MTD/recommended dose (RD) of IV XB002 alone or in combination over 18 months. The Cohort-Expansion Stage assessed preliminary efficacy through ORR using RECIST 1.1 (or RANO/PCWG3 criteria) over 12 months.
Other Endpoint	Safety and tolerability were evaluated via AEs/SAEs, treatment duration, and dose intensity over 30 months. Pharmacokinetics (Cmax, Ctrough) and immunogenicity (ADA) of XB002, total antibody, and free payload were analyzed. Anti-tumor activity was measured by ORR, DOR, and PFS (RECIST 1.1/RANO/PCWG3) through investigator/BIRC assessments. Overall survival was tracked in expansion cohorts for 12 months.    Click to Show/Hide

Ref 1	Preclinical Characterization of XB002, an Anti-Tissue Factor Antibody-Drug Conjugate for the Treatment of Solid Tumors
Ref 2	Study of XB002 in Subjects With Solid Tumors (JEWEL-101)