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FDA Approves Zanubrutinib for Waldenström’s Macroglobulinemia

This novel, small molecule inhibitor of Bruton's tyrosine kinase, was investigated in ASPEN study that compared zanubrutinib and ibrutinib in patients with MYD88 L265P mutation
03 Sep 2021
Targeted Therapy
Lymphomas

On 31 August 2021, the US Food and Drug Administration (FDA) approved zanubrutinib (Brukinsa, BeiGene) for adult patients with Waldenström’s macroglobulinemia (WM).

Zanubrutinib was investigated in ASPEN (NCT03053440), a randomised, active control, open-label study, comparing zanubrutinib and ibrutinib in patients with MYD88 L265P mutation (MYD88MUT) WM. Patients in Cohort 1 (n=201) were randomised 1:1 to receive zanubrutinib 160 mg twice daily or ibrutinib 420 mg once daily until disease progression or unacceptable toxicity. Cohort 2 enrolled patients with MYD88 wild-type (MYD88WT) or MYD88 mutation unknown WM (n=26 and 2, respectively) and received zanubrutinib 160 mg twice daily.

The major efficacy outcome used to support approval was response rate defined as partial response or better as assessed by an independent review committee (IRC) based on standard consensus response criteria from the International Workshop on Waldenström’s Macroglobulinemia-6. An additional efficacy outcome measure was duration of response (DoR).

Approval was based on a non-comparative assessment of response and DoR from the zanubrutinib arms. The response rate was 77.5% (95% confidence interval [CI] 68.1, 85.1) in the zanubrutinib arm. Event-free DoR at 12 months was 94.4% (95% CI 85.8, 97.9) in the zanubrutinib arm. In Cohort 2, response as assessed by IRC was seen in 50% (13 out of 26 response evaluable patients; 95% CI 29.9, 70.1).

The most common adverse reactions, including laboratory abnormalities, (≥20%) reported with zanubrutinib are neutrophil count decreased, upper respiratory tract infection, platelet count decreased, rash, haemorrhage, musculoskeletal pain, haemoglobin decreased, bruising, diarrhoea, pneumonia, and cough.

The recommended zanubrutinib dosage is 160 mg orally twice daily or 320 mg orally once daily.

Full prescribing information for Brukinsa is available here.

This review used the Assessment Aid, a voluntary submission from the applicant to facilitate the FDA’s assessment.

This application was granted fast track designation and orphan designation.

Healthcare professionals should report all serious adverse events suspected to be associated with the use of any medicine and device to FDA’s MedWatch Reporting System.

For assistance with single-patient INDs for investigational oncology products, healthcare professionals may contact FDA’s Oncology Center of Excellence Project Facilitate.

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