Celrixafor Plerixafor Injection 1.2ml

I. Basic Drug Information

Generic Name: Plerixafor Injection

Brand Names: Linuosheng / Shibeling / Celrixafor

Dosage Form: Solution for Injection

Specification: 1.2 mL: 24 mg (20 mg/mL)

Pharmacological Classification: CXCR4 Receptor Antagonist

Route of Administration: Subcutaneous Injection

Manufacturer: Celon Labs Ltd

II. Mechanism of Action

Plerixafor is a chemokine receptor antagonist. It acts by competitively binding to and blocking the CXCR4 receptor, thereby interfering with its interaction with the ligand SDF-1. This action blocks the "anchoring" signals from bone marrow stromal cells to hematopoietic stem cells, thereby promoting the release of hematopoietic stem cells from the bone marrow into the peripheral blood circulation to facilitate their collection.

III. Indications

Used in combination with G-CSF to mobilize hematopoietic stem cells into the peripheral blood in patients with Non-Hodgkin Lymphoma (NHL) and Multiple Myeloma (MM), in preparation for autologous hematopoietic stem cell transplantation.

IV. Dosage and Administration

Route of Administration: Subcutaneous injection.

Combination Regimen: Patients must first receive G-CSF therapy (10 μg/kg/day) for 4 days before initiating Plerixafor treatment.

Timing of Administration: Administer 11 hours prior to each scheduled hematopoietic stem cell collection.

Standard Dose: Calculated based on body weight at 0.24 mg/kg/day; the maximum daily dose must not exceed 40 mg.

Body Weight ≤ 83 kg: A fixed dose of 20 mg may be used, or the dose may be calculated based on body weight.

Body Weight > 83 kg: Calculate the dose based on body weight.

Duration of Treatment: Administer for a maximum of 4 consecutive days.

V. Important Dosage Adjustments: Patients with Renal Impairment

Renal function is a critical factor influencing Plerixafor dosage; a dose reduction is required for patients with a creatinine clearance (CLcr) ≤ 50 mL/min. Renal Function Status (CLcr) | Patient Weight | Recommended Dose

Normal (>50 mL/min) | ≤ 83 kg | 20 mg or 0.24 mg/kg/day

> 83 kg | 0.24 mg/kg/day (Maximum 40 mg/day)

Moderate to Severe Impairment (≤50 mL/min) | ≤ 83 kg | 13 mg or 0.16 mg/kg/day

> 83 kg | 0.16 mg/kg/day (Maximum 27 mg/day)

VI. Warnings and Precautions

1.  Severe Hypersensitivity Reactions: Severe hypersensitivity reactions, including anaphylactic shock, may occur. Patients should be observed for at least 30 minutes following administration, and the product should be used in a setting where emergency resuscitation equipment is available.

2.  Splenomegaly and Splenic Rupture: Post-marketing reports of splenomegaly and splenic rupture have been received. Patients should be monitored for signs of left upper quadrant abdominal pain, shoulder pain, or scapular pain.

3.  Potential Risk of Mobilizing Malignant Cells: Plerixafor carries a potential risk of mobilizing malignant cells in patients with hematologic malignancies; therefore, it is not indicated for use in patients with leukemia.

4.  Hematologic Changes: The drug may cause leukocytosis and decreased platelet counts; complete blood counts should be monitored.

5.  Vasovagal Reactions: Syncope or orthostatic hypotension may occur following injection; appropriate precautions should be taken.

VII. Adverse Reactions

Very Common (≥10%): Diarrhea, nausea, fatigue, injection site reactions, headache, arthralgia, dizziness, vomiting.

Common: Abdominal pain, hyperhidrosis, abdominal distension, insomnia, etc.

Serious Adverse Reactions: Hypersensitivity reactions, splenic rupture, myocardial infarction (rare).

VIII. Contraindications

Contraindicated in patients with a known hypersensitivity to plerixafor or to any of the excipients in the formulation.

IX. Drug Interactions

Based on *in vitro* study data, plerixafor is unlikely to be involved in drug interactions mediated by the cytochrome P450 enzyme system.

X. Use in Specific Populations

Pregnancy: Based on its mechanism of action, the drug may cause fetal harm. Use only when the potential benefits outweigh the risks.

Lactating Women: It is not known whether this drug is excreted in breast milk; therefore, caution should be exercised.

Pediatric Patients: The safety and efficacy of this product in patients under 18 years of age have not been established.

Geriatric Patients: No dosage adjustment is required for elderly patients with normal renal function. However, as the risk of impaired renal function is higher in the elderly population, the drug should be administered with caution.

XI. Storage

Storage Temperature: 2°C to 8°C (Refrigerate; do not freeze).

Protection from Light: Store in the original carton to protect from light.

Do Not Freeze: Freezing may cause precipitation or structural degradation of the drug; if the product becomes frozen, it must not be used.

Summary of Key Points

Plerixafor is an injectable agent used for mobilization prior to autologous hematopoietic stem cell transplantation; it must be used sequentially in combination with G-CSF. The dosage must be strictly individualized based on the patient's body weight and renal function, particularly for patients with renal impairment. During administration, clinicians should remain alert to potential risks such as severe hypersensitivity reactions and splenic rupture, and the drug should be administered under monitored conditions.

Product Specifications

Product Name: Plerixafor Injection 1.2 mL: 24 mg (Celrixafor)

Common Name: Plerixafor Injection

Composition: Plerixafor

Dosage Form: Solution for Injection

Specification: 1.2 mL: 24 mg (20 mg/mL)

Manufacturer: Celon Labs Ltd

Indications: Used in combination with G-CSF to mobilize hematopoietic stem cells into the peripheral blood in patients with Non-Hodgkin Lymphoma (NHL) and Multiple Myeloma (MM), to facilitate subsequent autologous hematopoietic stem cell transplantation.

Dosage and Administration:

Route of Administration: Subcutaneous injection.

Combination Regimen: Patients must first receive G-CSF therapy (10 µg/kg/day) for 4 days before initiating Plerixafor treatment.

Timing of Administration: Administer by injection 11 hours prior to each scheduled apheresis (hematopoietic stem cell collection) session.

Standard Dosage: Calculated based on body weight at 0.24 mg/kg/day; the maximum daily dose must not exceed 40 mg.

Body Weight ≤ 83 kg: A fixed dose of 20 mg may be used, or the dose may be calculated based on body weight. Body weight > 83 kg: Calculate based on body weight.

Course of treatment: Up to 4 consecutive days.