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Overview

Pharmacokinetic and biodistribution studies were conducted in rats on a novel serine protease inhibitor, LEX 032, that was radiolabeled with 131I by the Bolton-Hunter reagent. LEX 032, a genetically engineered recombinant human nonglycosylated serpin, has been shown to have antiinflammatory properties in a number of animal models of inflammation and reperfusion injury. When 131I-LEX 032 was injected intravenously, a rapid whole body clearance of radioactivity was seen. Blood clearance followed a similar pattern. Forty-eight hours postinjection, 2.00 +/- 0.65 of the administered dose remained in the body. Greater than 59% of the radio-activity was excreted in the urine within the first 24 hr. Little radioactivity was found in the feces. With the exception of the thyroid, no significant organ-related uptake was noted. Radioactivity in the liver peaked at 20 min postinjection, with 1.00 +/- 0.13% administered dose/g and approximately 10% administered dose in the whole liver. At 1 hr, uptake in the kidney (9.30 +/- 1.52% administered dose/g) was the highest among all tissues, except for the thyroid. Gamma camera images were consistent with the biodistribution pattern. Pharmacokinetics and biodistribution were not affected by the dose of LEX 032 and were quite different from those of glycosylated wild type antichymotrypsin. These data indicate that LEX 032 exhibits the pharmacokinetics expected of a nonglycosylated 45 kDa protein.

Drug Metabolism and Disposition

Biodistribution and Pharmacokinetics of 131I-Labeled LEX 032, A Recombinant Hybrid of Antichymotrypsin

Author: Michael Donegan ; Gulnur A. Elove ; Jirguhua Li ; Hemender R. Kolan ; Howard Sands ; Mathew L. Thakur ; Ramana Duggaraju

Pharmacokinetic and biodistribution studies were conducted in rats on a novel serine protease inhibitor, LEX 032, that was radiolabeled with 131I by the Bolton-Hunter reagent. LEX 032, a genetically engineered recombinant human nonglycosylated serpin, has been shown to have antiinflammatory properties in a number of animal models of inflammation and reperfusion injury. When 131I-LEX 032 was injected intravenously, a rapid whole body clearance of radioactivity was seen. Blood clearance followed a similar pattern. Forty-eight hours postinjection, 2.00 +/- 0.65 of the administered dose remained in the body. Greater than 59% of the radio-activity was excreted in the urine within the first 24 hr. Little radioactivity was found in the feces. With the exception of the thyroid, no significant organ-related uptake was noted. Radioactivity in the liver peaked at 20 min postinjection, with 1.00 +/- 0.13% administered dose/g and approximately 10% administered dose in the whole liver. At 1 hr, uptake in the kidney (9.30 +/- 1.52% administered dose/g) was the highest among all tissues, except for the thyroid. Gamma camera images were consistent with the biodistribution pattern. Pharmacokinetics and biodistribution were not affected by the dose of LEX 032 and were quite different from those of glycosylated wild type antichymotrypsin. These data indicate that LEX 032 exhibits the pharmacokinetics expected of a nonglycosylated 45 kDa protein.

Drug Metabolism and Disposition

Biodistribution and pharmacokinetics of I-labeled LEX 032, a recombinant hybrid of antichymotrypsin

Author: Li, Jirguhua ; Donegan, Michael ; Duggaraju, Ramana ; Thakur, Mathew L. ; Kolan, Hemender R. ; Sands, Howard ; Elove, Gulnur A.

Pharmacokinetic and biodistribution studies were conducted in rats on a novel serine protease inhibitor, LEX 032, that was radiolabeled with ¹³¹I by the Bolton-Hunter reagent.LEX 032, a genetically engineered recombinant human nonglycosylated serpin, has been shown to have antiinflammatory properties in a number of animal models of inflammation and reperfusion injury.When ¹³¹I-LEX 032 was injected i.v., a rapid whole body clearance of radioactivity was seen.Blood clearance followed a similar pattern.Forty-eight hours postinjection, 200 ± 0.65% of the administered dose remained in the body.Greater than 59% of the radioactivity was excreted in the urine within the first 24 h.Little radioactivity was found in the feces.With the exception of the thyroid, no significant organ-related uptake was noted.Radioactivity in the liver peaked at 20 min postinjection, with 1.00 ± 0.13% administered dose/g and ∼10% administered dose in the whole liver.At 1 h, uptake in the kidney (9.30 ± 1.52% administered dose/g) was the higher among all tissues, except for the thyroid.Gamma camera images were consistent with the biodistribution pattern.Pharmacokinetics and biodistribution were not affected by the dose of LEX 032 and were quite different from those of glycosylated wild type antichymotrypsin.These data indicate that LEX 032 exhibits the pharmacokinetics expected of a nonglycosylated 45 kDa protein.

100 Deals associated with Sparta Pharmaceuticals, Inc.

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100 Translational Medicine associated with Sparta Pharmaceuticals, Inc.

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Pipeline

Pipeline Snapshot as of 17 Nov 2024

The statistics for drugs in the Pipeline is the current organization and its subsidiaries are counted as organizations,Early Phase 1 is incorporated into Phase 1, Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3

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Current Projects

Drug(Targets)	Indications	Global Highest Phase

LEX-026 ( thrombin )	Thromboembolism More	Discontinued
LEX-032 ( CTSG x ELA2 x S1: Chymotrypsin x Serine protease )	Pancreatitis More	Discontinued
LEX-028 ( CTSG )	Inflammation More	Discontinued
LEX-043	Inflammation More	Pending