Drug Discovery

Acerta Pharma, in close collaboration with research groups in AstraZeneca, takes an innovative approach to discover, develop and deliver targeted novel transformational medicines for patients with hematological malignancies.

Acerta Pharma is a leader in the field of covalent binding technology and is applying this technology to create a range of highly selective therapies for cancer. We are advancing the scientific understanding of disease pathways in oncology through our extensive portfolio of investigational and approved agents, including our covalent BTK inhibitor CALQUENCE® (acalabrutinib).

Both at the level of research and development, Acerta scientists work closely with R&D colleagues from Acerta in the US (San Carlos and South San Francisco), and from AstraZeneca, including those from AstraZeneca in Cambridge (UK), Waltham (Boston, US) and Gaithersburg in the US, and Gothenburg in Sweden. Discovery project teams are collaborative with AstraZeneca groups which retain key capabilities which Acerta teams link into.

Innovative Clinical Studies

Working together, Acerta and AstraZeneca are focused on Innovative Clinical Strategies to enable us to combine our extensive oncology portfolio of cancer therapies as well as combinations with exciting, novel compounds in development at partner companies.

These combinations are based on strong scientific hypotheses (preclinical and clinical data) and delivered through innovative master protocols that enable us to evaluate multiple combinations of agents in the context of a single master protocol and answer more questions in less time to accelerate the delivery of effective therapeutic combinations to patients.

Innovative Clinical Trial Design
Innovative Clinical Trial Design

Resistance Biology

Acerta Pharma has deep expertise in innovative drug profiling technologies. Our multiparametric phospho-proteomic platform enables the characterization of activated signaling networks within complex tissues and in discrete cell subsets.

This exceptional capability reveals the impact of our drug candidates on tumor and non-tumor cell populations in clinically relevant tissues. In addition, we developed a novel assay that measures the level of binding of CALQUENCE to BTK. We used this target coverage assay to quickly establish the best dosing regimen, bringing CALQUENCE to patients faster.

CALQUENCE is a highly selective inhibitor of BTK, a kinase in the B-cell receptor (BCR) signaling pathway, and a driving factor for B-cell malignancies. Matched blood samples from patients with chronic lymphocytic leukemia (CLL), collected before CALQUENCE therapy and after 6 months or at disease progression, offer a unique opportunity to explore the changes in CLL tumor biology under therapeutic pressure. Patient’s peripheral blood samples receive the most comprehensive set of analyses covering genomic, transcriptomic, proteomic, phospho-signaling, and ex-vivo drug sensitivity profiling. The goal is to identify signatures that correlate with disease and point to potential mechanisms of resistance. Altogether, BPACS is an unparalleled platform providing rationale for new combination therapies, as well as novel drug targets.

Translational Medicine

As therapies in development for hematological malignancies are aiming for deeper, more durable responses, assessing measurable residual disease (MRD) is becoming an essential part of clinical studies since MRD may be a predictor of duration of response (PFS/OS).

Our Translational Medicine (TM) team is actively implementing MRD endpoints in our clinical trials to understand what treatments can drive MRD to undetectable levels. To support this, the TM team is evaluating several methods, including flow cytometry and DNA-based MRD assays, to measure MRD in heme indications.

BTK Overview

BTK plays a key role in the B-cell receptor, or BCR, pathway which regulates the development, function, and survival of the B cell.


Acalabrutinib is a highly selective, Bruton's tyrosine kinase (BTK) inhibitor.