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Table 4 AUC values (%ID/g h) and therapeutic ratios of 131I-, 90Y-CHX-A″ DTPA- and 177Lu-CHX-A″ DTPA-labelled hu3S193 antibody variants in A431 tumour-bearing mice

From: Engineering anti-Lewis-Y hu3S193 antibodies with improved therapeutic ratio for radioimmunotherapy of epithelial cancers

Radiolabel

Antibody

AUCtumour

AUCblood

AUCliver

AUCkidney

T/La

T/Kb

T/Bc

90Y-CHX-A" DTPA-

Wild type

2849

1276

498

636

5.7

4.5

2.2

 

H435A

2168

964

514

561

4.2

3.9

2.3

 

I253A

1541

1126

738

633

2.1

2.4

1.4

 

H310A

1506

559

676

482

2.2

3.1

2.7

 

I253A/H310A

1037

418

1037

412

1.0

2.5

2.5

177Lu-CHX-A" DTPA-

Wild type

5203

1709

833

1265

6.3

4.1

3.1

 

H435A

4076

1235

835

932

4.9

4.4

3.3

 

I253A

3514

1362

1189

1029

3.0

3.4

2.6

 

H310A

2400

783

1104

774

2.2

3.1

3.1

 

I253A/H310A

2699

453

1421

539

1.9

5.0

6.0

131I-

Wild type

2739

2085

560

659

4.9

4.2

1.3

 

H435A

679

516

129

175

5.2

3.9

1.3

 

I253A

568

516

141

159

4.0

3.6

1.1

 

H310A

655

439

118

125

5.5

5.2

1.5

 

I253A/H310A

602

422

107

120

5.6

5.0

1.4

  1. aT/L, AUCtumour-to-AUCliver ratio
  2. bT/K, AUCtumour-to-AUCkidney ratio
  3. cT/B, AUCtumour-to-AUCblood ratio