ACIVICIN

NSC - 163501

Acivicin is currently available from both the National Cancer
Institute and from the Upjohn Company of Kalamazoo, Michigan
for clinical trials sponsored by the Division of Cancer Treatment,
National Cancer Institute. Information relevant to both products
is provided below.

SMILES: N[C@@H]([C@@H]1CC(=NO1)Cl)C(=O)O

Chemical Name: a-Amino-3-chloro-4,5-dihydro-5-isoxazoleaceticacid,[S- (R *,R *)]-

Other Names: AT-125, U-42126, Acivicin (USAN)

CAS Registry Number: 42228-92-2

Molecular Formula: C5H7ClN2O3     M.W.: 178.6

How Supplied: NSC - 603071 Injection, 5 mg, ampule: 5 mg/mL
concentrate, 1 mL, in dimethylacetamide,
1 mL/amber ampule.

Special Diluent: NSC - 651935 Vial: Polyethylene Glycol 400,
51%, with 0.01 Molar Phosphoric Acid
Buffer, 49 %, 49 mL/amber vial.

Solution Preparation: Add one milliliter of the 9-amino-
camptothecin/dimethylacetamide concentrate (use a glass
syringe) to the amber vial containing 49 milliliters of special
diluent.

The resulting mixture contains 100 micrograms of 9-
aminocamptothecin per milliliter in a 2% dimethylacetamide
(v/v), 50% polyethylene glycol 400 (v/v), and 48% 0.01 M
phosphoric acid (v/v) solution, 50 mL per vial. Filter the final
solution through a 5 micron filter. Use within 28 hours.

Note: Contact of the undiluted 9-aminocamptothecin/
dimethylacetamide concentrate with plastic items, including
filters and syringes, should be avoided.

Further dilution of the 100 mcg/mL solution with 0.9% Sodium
Chloride Injection must be targeted to a concentration of <= one
microgram/mL as precipitation will occur at higher
concentrations. Dilutions containing 0.1 to 1 mcg/mL of 9-
aminocamptothecin in 0.9% Sodium Chloride Injection are
stable for 28 hours. Those in 5% Dextrose Injection are less
stable; this should not be used. These solutions may be prepared
in PVC or polyolefin containers.

Caution: 9-aminocamptothecin is intended for appropriate
syringe pump administration only. The drug is not compatible
with standard infusion fluids and therefore cannot be further
diluted (except as noted in the previous paragraph) nor can it be
piggybacked into an existing I.V. line port. Additional special
diluent is available to facilitate larger doses and to flush central
venous catheters to displace any aqueous solution present.

Storage: Store the intact ampules under refrigeration (2-8 °C).
Stability: Shelf-life surveillance of the ampules and vials is
ongoing.

Constitution as recommended results in a solution
which is chemically and physically stable in the amber
diluent vial for at least 28 hours stored at refrigerated
temperature (2-8 °C).

Route of Administration: Intravenous