The main ingredient of this product is bortezomib.

Chemical name: [(1R)-3-methyl-1-[[(2S)-1-oxo-3-phenyl-2-[(pyrazinylcarbonyl) amino] propyl] amino] butyl] boronic acid.

Structural Formula:

Molecular formula: C₁₉H₂₅BN₄O₄

Molecular weight:  384.24 

Excipients: mannitol, nitrogen.

This product is a white or off-white powder or a cake. 

Multiple Myeloma

This product in combination with melphalan and prednisone (MP regimen) is indicated for the treatment in patients with previously untreated multiple myeloma and are not suitable for high-dose chemotherapy and bone marrow transplantation. Single drug is indicated for the treatment in recurrent multiple myeloma patients who have received at least one or more treatments.

Mantle cell lymphoma

This product can be used in the treatment of patients with recurrent or refractory mantle cell lymphoma. This patient has received at least one treatment before using this product. The safety and efficacy data for this indication comes from a one-arm, phase II clinical study of a mantle cell lymphoma that has relapsed after prior treatment. [see Clinical Studies], there is still a lack of clinical research data for the Chinese population. 

This product is only for intravenous administration, and intrathecal injection can cause death. It is contraindicated in patients who are allergic to bortezomib, boron or mannitol.

Untreated multiple myeloma patients

This product is administered as a 3 to 5 second bolus intravenous injection when combined with oral melphalan and oral prednisone. Each cycle of treatment is 6 weeks (as shown in Table 1) for a total of 9 cycles. This product is administered twice a week (Days 1, 4, 8, 11, 22, 25, 29 and 32) during the first to fourth cycles. This product is administered once a week (Days 1, 8, 22 and 29) during the 5th to 9th cycles. At least 72 hours should elapse between consecutive doses of Bortezomib.

Recurrent multiple myeloma patients and recurrent mantle cell lymphoma patients

Single used

Recommended dosage

Bortezomib (1.3 mg/m2/dose) is administered twice weekly for 2 weeks (Days 1, 4, 8, and 11) followed by a 10-day rest period (Days 12-21). 3 weeks is a cycle of treatment and at least 72 hours should elapse between consecutive doses of Bortezomib. For extended therapy of more than 8 cycles, this product may be administered on the standard schedule or, for relapsed multiple myeloma, on a maintenance schedule of once weekly for 4 weeks (Days 1, 8, 15, and 22) followed by a 13-day rest period (Days 23 to 35).

Dose Modifications and restart treatment

Bortezomib therapy should be withheld at the onset of any Grade 3 non-hematological or Grade 4 hematological toxicities excluding neuropathy as discussed below. Once the symptoms of the toxicity have resolved, Bortezomib therapy may be reinitiated at a 25% reduced dose (1.3 mg/m2/dose reduced to 1 mg/m2/dose; 1 mg/m2/dose reduced to 0.7 mg/m2/dose).

If the patient has neuropathic pain or peripheral sensory neuropathy associated with the treatment of this product, it is recommended to use the modified dose recommended in the following tablet. The attending physician should select the appropriate dose adjustment plan according to the actual condition of the patient. There are reports of interruption or discontinuation of treatment due to severe autonomic neuropathy. Patients with pre-existing severe neuropathy should be treated with Bortezomib only after careful risk-benefit assessment

Patents with hepatic impairment

Patients with mild hepatic impairment do not need to adjust the starting dose and should be treated at the recommended dose. The initial dose of this product should be reduced to 0.7 mg/m2 in patients with moderate and severe hepatic impairment. The subsequent treatment dose is increased to 1.0 mg/m2 or further reduced to 0.5 mg/m2 depending on the patient's first cycle tolerance.

Patients with renal impairment

The pharmacokinetics of this product is not affected by the degree of renal impairment. Therefore, dosing adjustments of this product are not necessary for patients with renal insufficiency. Since dialysis will reduce the concentration of this product, it should be administered after the dialysis procedure.

Administration

This product should be completely dissolved in saline and then injected through a central venous catheter or peripheral vein within 3 to 5 seconds, followed by a 0.9% sodium chloride solution for injection.

Note: Please refer to the product manual for details.