Related Experiment Video
Updated: Oct 17, 2026

Scaled-Up Preparation of an Intermediate of Upatinib, ACT051-3
Published on: April 7, 2023
Rocbrutinib: First Approval
1Springer Nature, Private Bag 65901, Mairangi Bay, Auckland, 0754, New Zealand. dru@adis.com.
Abstract:
Rocbrutinib (; LP-168) is a fourth generation Bruton's tyrosine kinase (BTK) inhibitor with both covalent and non-covalent modes of binding, which allow it to inhibit both wildtype as well as mutant variants of BTK. It is being developed by Lupeng Pharmaceuticals primarily as a treatment for patients with B-cell malignancies. Rocbrutinib received its first approval in June 2026 in China for use in adult patients with mantle cell lymphoma (MCL) that is relapsed or refractory to BTK inhibitors, and who have received ≥ 2 systemic therapies (including BTK inhibitors). This article summarizes the milestones in the development of rocbrutinib leading to its first approval in this indication.
Related Concept Videos
FDA Approved Drugs: Changes to Approved Drugs
Treatment Resistant Cancers
Treatment for Pulmonary Arterial Hypertension: Receptor Tyrosine Kinase Inhibitors and Calcium Channel Blockers
TKIs, such as imatinib (Gleevec), are particularly effective in tackling the growth and mitogenic factors that become upregulated in PAH patients. These factors contribute to the...
Prescription, Nonprescription and Orphan Drugs
The misuse and addiction to prescription drugs is a growing problem that can affect people of all age groups, specifically teenagers. This can happen when prescription medications are used in ways not intended by the prescriber, such as taking someone else's prescription or using medication for...
Targeted Cancer Therapies
There are several types of targeted therapies against specific...
Drug Products: Biologics, Biosimilars and Interchangeables