Name | Zanubrutinib |
CAS number | 1691249-45-2 |
Description | Zanubrutinib (BGB-3111) is a potent, selective, and irreversible Bruton's tyrosine kinase (BTK) inhibitor with demonstrated efficacy both in vitro and in vivo. In vitro, it effectively inhibits BTK activity with an IC₅₀ of approximately 0.35 nM, showing high selectivity over other kinases such as EGFR and ITK, and minimal off-target effects on kinases like JAK3. In vivo, zanubrutinib has shown significant therapeutic potential in animal models of hematological malignancies, including mantle cell lymphoma, where it effectively suppressed tumor growth and improved survival rates. Additionally, it has demonstrated efficacy in models of pulmonary fibrosis and cardiac fibrosis, attenuating disease progression through mechanisms involving inhibition of TGF-β1/Smad and TGF-β1/mTOR signaling pathways. |
Related CAS | 1633350-06-7 (racemate) 1691249-45-2 (S-isomer) 1691249-44-1 (R-isomer) |
Synonym | BGB-3111; BGB 3111; BGB3111; Zanubrutinib; Brukinsa. |
Appearance | Solid powder |
Quality Standard | USP, EP, BP, CP |
Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
Storage Condition | Dry, dark and at 0 - 4 ℃ for short term (days to weeks) or -20 ℃ for long term (months to years). |
Shelf Life | >2 years if stored properly |
Sample package | Aluminium foil bag |
Commercial package | Aluminium Tin, Fiber drum |
Origin | China |
Zanubrutinib More Info
Zanubrutinib (brand name: Brukinsa®) is a next-generation, orally administered covalent Bruton’s tyrosine kinase (BTK) inhibitor designed for targeted treatment of B-cell malignancies, developed by BeiGene and commercialized globally in partnership with Bristol-Myers Squibb (BMS) in key markets 。
Key Profile
Mechanism of Action: Covalently binds to the active site of BTK, blocking B-cell receptor (BCR) signaling critical for proliferation, survival, and trafficking of malignant B cells; improved selectivity vs. first-generation BTK inhibitors to reduce off-target effects 。
Formulation & Dosing: Oral capsules/tablets; typical regimens: 160 mg twice daily or 320 mg once daily (oral, with/without food), continued until disease progression or unacceptable toxicity 。
Key Indications (FDA/EMA/WHO-relevant, as of 2025):
Chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL) (monotherapy) 。
Waldenström’s macroglobulinemia (WM) (monotherapy) 。
Mantle cell lymphoma (MCL): Previously treated adults (accelerated approval based on ORR; confirmatory trials ongoing) 。
Marginal zone lymphoma (MZL): Relapsed/refractory (R/R) adults with prior anti-CD20-based therapy (accelerated approval based on ORR) 。
Follicular lymphoma (FL): R/R adults with ≥2 prior lines, in combination with obinutuzumab (accelerated approval based on response rate/durability) 。
Approval Milestones: First approved in the U.S. (Nov 2019, MCL), followed by China (2020) and EU/Japan/other regions; listed on WHO Essential Medicines List (EML) for CLL/SLL, recognizing its public health value 。
Clinical Highlights: Phase 3 trials (e.g., ASPEN for WM, ALPINE for CLL/SLL) demonstrated favorable efficacy (higher ORR, deeper responses) and safety (lower rates of atrial fibrillation, hypertension, bleeding vs. ibrutinib), supporting its role as a preferred BTK inhibitor in many settings 。
Safety Profile: Common adverse events include neutropenia, thrombocytopenia, diarrhea, fatigue, and upper respiratory tract infections; monitoring for infections, bleeding, arrhythmias, and second primary malignancies is recommended per prescribing information 。
Global Access & Partnerships: Commercialized by BeiGene in China and select markets; co-commercialized with BMS in the U.S., EU, Japan, and other major territories to expand global reach 。
Brief Clinical Context
Zanubrutinib has become a cornerstone in the treatment of B-cell malignancies, offering a well-tolerated oral option for both frontline and relapsed/refractory settings. Its inclusion in WHO EML underscores its importance in improving access to effective targeted therapy for CLL/SLL globally. Ongoing trials explore combinations with anti-CD20 mAbs, BCL2 inhibitors, and other agents to further enhance outcomes and expand indications.
