ADC ID	DRG0QBUOH
ADC Name	GLK-33
Synonyms	GLK-33    Click to Show/Hide
Organization	Glykos Finland Oy.; University of Helsinki.; Finnish Cancer Institute.; University of Turku.; Helsinki University Hospital Comprehensive Cancer Center.
Drug Status	Investigative
Drug-to-Antibody Ratio	8
Structure
Antibody Name	Lintuzumab					Antibody Info
Antigen Name	Myeloid cell surface antigen CD33 (CD33)					Antigen Info
Payload Name	Glucuronyl-monomethyl-auristatin E (MMAU)					Payload Info
Therapeutic Target	Microtubule (MT)					Target Info
Linker Name	Undisclosed
Conjugate Type	Random conjugation through nucleophilic lysines

Standard Type	Value	Units	Description	Reference
Maximum Observed Concentration (Cmax)	665	ug/mL	Pharmacokinetic parameters of CLK-33 in single iv dose in Sprague-Dawley rats.	[1]
Area Under the Concentration-Time Curve (AUC)	1577	day&#42ug/mL	Pharmacokinetic parameters of CLK-33 in single iv dose in Sprague-Dawley rats.	[1]
Maximum Observed Concentration (Cmax)	665	ug/mL	Pharmacokinetic parameters of CLK-33 in single iv dose in mouse HL-60 tumor models. 20 mg/kg.	[1]
Area Under the Concentration-Time Curve (AUC)	1577	day&#42ug/mL	Pharmacokinetic parameters of CLK-33 in single iv dose in mouse HL-60 tumor models. 20 mg/kg.	[1]

Standard Type	Value	Units	Description	Reference
Area Under the Concentration-Time Curve (AUC)	1577	day&#42ug/mL	Pharmacokinetic parameters of CLK-33 in single iv dose in Sprague-Dawley rats.	[1]
Area Under the Concentration-Time Curve (AUC)	1577	day&#42ug/mL	Pharmacokinetic parameters of CLK-33 in single iv dose in mouse HL-60 tumor models. 20 mg/kg.	[1]

Standard Type	Value	Units	Description	Reference
Area Under the Concentration-Time Curve (AUC)	1577	day&#42ug/mL	Pharmacokinetic parameters of CLK-33 in single iv dose in Sprague-Dawley rats.	[1]
Area Under the Concentration-Time Curve (AUC)	1577	day&#42ug/mL	Pharmacokinetic parameters of CLK-33 in single iv dose in mouse HL-60 tumor models. 20 mg/kg.	[1]

Standard Type	Value	Units	Description	Reference
Area Under the Concentration-Time Curve (AUC)	1577	day&#42ug/mL	Pharmacokinetic parameters of CLK-33 in single iv dose in Sprague-Dawley rats.	[1]
Elimination Half-Life (t1/2)	5.3	d	Pharmacokinetic parameters of CLK-33 in single iv dose in Sprague-Dawley rats.	[1]
Area Under the Concentration-Time Curve (AUC)	1577	day&#42ug/mL	Pharmacokinetic parameters of CLK-33 in single iv dose in mouse HL-60 tumor models. 20 mg/kg.	[1]
Elimination Half-Life (t1/2)	5.3	d	Pharmacokinetic parameters of CLK-33 in single iv dose in mouse HL-60 tumor models. 20 mg/kg.	[1]

Standard Type	Value	Units	Cell Line	Disease Model
Half Maximal inhibitory Concentration (lC50)	0.14	nM	CVCL_0064	Childhood acute monocytic leukemia
Half Maximal inhibitory Concentration (lC50)	0.21	nM	CVCL_2119	Adult acute myeloid leukemia
Half Maximal inhibitory Concentration (lC50)	0.24	nM	CVCL_0002	Acute myeloblastic leukemia with maturation, Adult acute myeloid leukemia with maturation
Half Maximal inhibitory Concentration (lC50)	1.4	nM	CVCL_0374	Adult acute myeloid leukemia
Half Maximal inhibitory Concentration (lC50)	2.7	nM	CVCL_2149	Acute myeloid leukemia
Half Maximal inhibitory Concentration (lC50)	725	nM	CVCL_0004	Chronic myelogenous leukemia
Half Maximal inhibitory Concentration (lC50)	> 1000	nM	CVCL_0008	Burkitt lymphoma
Half Maximal inhibitory Concentration (lC50)	> 1000	nM	CVCL_0597	Burkitt lymphoma

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.14 nM	Positive CD33 expression (CD33+++/++)
Method Description	GLK-33 exhibited remarkable efficacy in reducing cell viability within CD33-positive leukemia cell lines.
In Vitro Model	Childhood acute monocytic leukemia	MV4-11 cells		CVCL_0064
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.21 nM	Positive CD33 expression (CD33+++/++)
Method Description	GLK-33 exhibited remarkable efficacy in reducing cell viability within CD33-positive leukemia cell lines.
In Vitro Model	Adult acute myeloid leukemia	MOLM-13 cells		CVCL_2119
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.24 nM	Positive CD33 expression (CD33+++/++)
Method Description	GLK-33 exhibited remarkable efficacy in reducing cell viability within CD33-positive leukemia cell lines.
In Vitro Model	Acute myeloblastic leukemia with maturation, Adult acute myeloid leukemia with maturation	HL60 cells		CVCL_0002
Experiment 4 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.4 nM	Positive CD33 expression (CD33+++/++)
Method Description	GLK-33 exhibited remarkable efficacy in reducing cell viability within CD33-positive leukemia cell lines.
In Vitro Model	Adult acute myeloid leukemia	KG-1 cells		CVCL_0374
Experiment 5 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	2.7 nM	Positive CD33 expression (CD33+++/++)
Method Description	GLK-33 exhibited remarkable efficacy in reducing cell viability within CD33-positive leukemia cell lines.
In Vitro Model	Acute myeloid leukemia	OCI-M1 cells		CVCL_2149
Experiment 6 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	725 nM	Positive CD33 expression (CD33+++/++)
Method Description	GLK-33 exhibited remarkable efficacy in reducing cell viability within CD33-positive leukemia cell lines.
In Vitro Model	Chronic myelogenous leukemia	K-562 cells		CVCL_0004
Experiment 7 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 1000 nM	Negative CD33 expression (CD33-)
Method Description	GLK-33 exhibited remarkable efficacy in reducing cell viability within CD33-positive leukemia cell lines.
In Vitro Model	Burkitt lymphoma	Daudi cells		CVCL_0008
Experiment 8 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 1000 nM	Negative CD33 expression (CD33-)
Method Description	GLK-33 exhibited remarkable efficacy in reducing cell viability within CD33-positive leukemia cell lines.
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597

Ref 1	Targeting CD33+ Acute Myeloid Leukemia with GLK-33, a Lintuzumab-Auristatin Conjugate with a Wide Therapeutic Window