Plerixafor Injection

This article is compiled based on the United States Pharmacopeia (USP) – 2025 Edition

Issued and maintained by the United States Pharmacopeial Convention (USP)

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1 DEFINITION

Plerixafor Injection is a sterile isotonic solution of Plerixafor in Water for Injection. It contains NLT 90.0% and NMT 110.0% of the labeled amount of plerixafor (C₂₈H₅₄N₈) with no preservatives.

2 IDENTIFICATION

A. The UV spectrum of the plerixafor peak of the Sample solution corresponds to that of the Standard solution, as obtained in the Assay.

B. The retention time of the major peak of the Sample solution corresponds to that of the Standard solution, as obtained in the Assay.

3 ASSAY

Procedure

Solution A: Methanol and water (8.5: 91.5). To each liter of the solution, add 1 mL of trifluoroacetic acid.

Solution B: Methanol and water (50:50). To each liter of the solution, add 1 mL of trifluoroacetic acid.

Mobile phase: See Table 1.

Table 1

Diluent: 0.05 N hydrochloric acid

Standard solution: 2 mg/mL of USP Plerixafor RS in Diluent. Sonicate to dissolve.

Sample solution: Nominally 2 mg/mL of plerixafor from Injection prepared as follows. Empty and pool the contents of a suitable number of vials into a suitable glass container to obtain NLT 22 mL of the solution. Mix and transfer 5 mL of the pooled sample into a 50-mL volumetric flask and dilute with Diluent to volume.

Chromatographic system

(See Chromatography 〈621〉, System Suitability.)

Mode: LC

Detector: UV 230 nm. For Identification A, use a diode array detector in the range of 200–400 nm.

Column: 4.6-mm × 25-cm; 5-μm packing L1

Column temperature: 45°

Flow rate: 1 mL/min

Injection volume: 10 μL

System suitability

Sample: Standard solution

Suitability requirements

Tailing factor: NMT 6.0

Relative standard deviation: NMT 2.0%

Analysis

Samples: Standard solution and Sample solution

Calculate the percentage of the labeled amount of plerixafor (C₂₈H₅₄N₈) in the portion of Injection taken:

Result = (r_U/r_S) × (C_S/C_U) × 100

r_U = peak response of plerixafor from the Sample solution

r_S = peak response of plerixafor from the Standard solution

C_S = concentration of USP Plerixafor RS in the Standard solution (mg/mL)

C_U = nominal concentration of plerixafor in the Sample solution (mg/mL)

Acceptance criteria: 90.0%–110.0%

4 IMPURITIES

Organic Impurities

Solution A, Solution B, Mobile phase, Diluent, Sample solution, and Chromatographic system: Proceed as directed in the Assay.

System suitability solution: 2 mg/mL of USP Plerixafor System Suitability Mixture RS in Diluent. Sonicate to dissolve.

Standard solution: 0.004 mg/mL of USP Plerixafor RS in Diluent

Sensitivity solution: 0.002 mg/mL of USP Plerixafor RS in Diluent from the Standard solution

System suitability

Samples: System suitability solution, Standard solution, and Sensitivity solution

[Note - Plerixafor 4-benzyl analog and plerixafor 8-benzyl analog coelute under these chromatographic conditions. The relative retention times in Table 2 are provided as information that could aid in peak assignment.]

Table 2

^a{4-[(1,4,8,11-Tetraazacyclotetradecan-1-yl)methyl]phenyl}methanol.

^b 1,4-Bis{4-[(1,4,8,11-tetraazacyclotetradecan-1-yl)methyl]benzyl}-1,4,8,11-tetraazacyclotetradecane.

^c 1,8-Bis{4-[(1,4,8,11-tetraazacyclotetradecan-1-yl)methyl]benzyl}-1,4,8,11-tetraazacyclotetradecane.

^d 1,11-Bis{4-[(1,4,8,11-tetraazacyclotetradecan-1-yl)methyl]benzyl}-1,4,8,11-tetraazacyclotetradecane.

Suitability requirements

Resolution: NLT 1.0 between plerixafor and plerixafor benzyl alcohol, System suitability solution

Relative standard deviation: NMT 2.0%, Standard solution

Signal-to-noise ratio: NLT 10, Sensitivity solution

Analysis

Samples: Standard solution and Sample solution

Calculate the percentage of any unspecified degradation product in the portion of Injection taken:

Result = (r_U/r_S) × (C_S/C_U) × F × 100

r_U = peak response of any unspecified degradation product from the Sample solution

r_S = peak response of plerixafor from the Standard solution

C_S = concentration of USP Plerixafor RS in the Standard solution (mg/mL)

C_U = nominal concentration of plerixafor in the Sample solution (mg/mL)

F = relative response factor (see Table 3)

Acceptance criteria: See Table 3. The reporting threshold is 0.1%.

Table 3

5 SPECIFIC TESTS

Bacterial Endotoxins Test 〈85〉: Meets the requirements

Sterility Tests 〈71〉: Meets the requirements

pH 〈791〉: 6.0–7.5

Osmolality and Osmolarity 〈785〉: 270–310 mOsm/kg

Particulate Matter in Injections 〈788〉: Meets the requirements for small-volume injections

Requirements: Meets the requirements under Injections and Implanted Drug roducts 〈1〉, Product Quality Tests Common to Parenteral Dosage Forms, Universal Tests, Container Content

6 ADDITIONAL REQUIREMENTS

Packaging and Storage: Preserve in single-dose containers, preferably of Type I glass. Store at controlled room temperature.

USP Reference Standards 〈11〉

USP Plerixafor RS

USP Plerixafor System Suitability Mixture RS

Contains a mixture of the following 5 compounds:

Plerixafor.

Plerixafor 4-benzyl analog: 1,4-Bis{4-[(1,4,8,11-tetraazacyclotetradecan-1-yl)methyl]benzyl}-1,4,8,11-tetraazacyclotetradecane.

Plerixafor 8-benzyl analog: 1,8-Bis{4-[(1,4,8,11-tetraazacyclotetradecan-1-yl)methyl]benzyl}-1,4,8,11-tetraazacyclotetradecane.

Plerixafor 11-benzyl analog: 1,11-Bis{4-[(1,4,8,11-tetraazacyclotetradecan-1-yl)methyl]benzyl}-1,4,8,11-tetraazacyclotetradecane.

Plerixafor benzyl alcohol: {4-[(1,4,8,11-Tetraazacyclotetradecan-1-yl)methyl]phenyl}methanol.