Bioavailability, biotransformation, and excretion of the covalent bruton tyrosine kinase inhibitor acalabrutinib in rats, dogs, and humans
T Podoll, PG Pearson, J Evarts, T Ingallinera… - Drug Metabolism and …, 2019 - ASPET
Acalabrutinib is a targeted, covalent inhibitor of Bruton tyrosine kinase (BTK) with a unique 2-butynamide
warhead that has relatively lower reactivity than other marketed acrylamide …
warhead that has relatively lower reactivity than other marketed acrylamide …
Bridging in vitro dissolution and in vivo exposure for acalabrutinib. Part II. A mechanistic PBPK model for IR formulation comparison, proton pump inhibitor drug …
…, CM Krejsa, MA Andrew, TG Ingallinera… - European journal of …, 2019 - Elsevier
Acalabrutinib (Calquence®) 100 mg (bid) has received accelerated approval by FDA for the
treatment of adult patients with mantle cell lymphoma (MCL) who have received at least one …
treatment of adult patients with mantle cell lymphoma (MCL) who have received at least one …
[HTML][HTML] Nx-5948, a selective degrader of BTK with activity in preclinical models of hematologic and brain malignancies
…, R Rountree, M Tan, N Brathaban, T Ingallinera… - Blood, 2021 - Elsevier
Bruton's tyrosine kinase (BTK) plays a key role in cell survival in B cell malignancies, and
covalent inhibitors of BTK, such as ibrutinib and acalabrutinib, have proven efficacious in …
covalent inhibitors of BTK, such as ibrutinib and acalabrutinib, have proven efficacious in …
[HTML][HTML] Nx-2127, a degrader of BTK and IMiD neosubstrates, for the treatment of B-cell malignancies
…, M Noviski, J Ye, S Basham, T Ingallinera… - Blood, 2020 - Elsevier
Bruton's tyrosine kinase (BTK) plays a key role in cell survival in B cell malignancies, such
as chronic lymphocytic leukemia (CLL). Covalent inhibitors of BTK, such as ibrutinib and …
as chronic lymphocytic leukemia (CLL). Covalent inhibitors of BTK, such as ibrutinib and …
Bridging in vitro dissolution and in vivo exposure for acalabrutinib. Part I. Mechanistic modelling of drug product dissolution to derive a P-PSD for PBPK model input
…, A Blanazs, S Grover, TG Ingallinera… - European Journal of …, 2019 - Elsevier
Drug product dissolution for four batches of acalabrutinib 100 mg capsules were analyzed
with in vitro dissolution in various pH conditions and in media containing synthetic surfactant …
with in vitro dissolution in various pH conditions and in media containing synthetic surfactant …
Multi-layered analyses using directed partitioning to identify and discriminate between biogenic amines
TL Nelson, I Tran, TG Ingallinera, MS Maynor… - Analyst, 2007 - pubs.rsc.org
Multiple layers of statistical analyses were used to decipher the response from a single,
cross-reactive conjugated polymer (1) providing enhanced classification accuracies over …
cross-reactive conjugated polymer (1) providing enhanced classification accuracies over …
Discovery and Preclinical Pharmacology of NX-2127, an Orally Bioavailable Degrader of Bruton's Tyrosine Kinase with Immunomodulatory Activity for the Treatment of …
…, MC Clifton, S Gajewski, TG Ingallinera… - Journal of Medicinal …, 2024 - ACS Publications
Bruton’s tyrosine kinase (BTK), a member of the TEC family of kinases, is an essential effector
of B-cell receptor (BCR) signaling. Chronic activation of BTK-mediated BCR signaling is a …
of B-cell receptor (BCR) signaling. Chronic activation of BTK-mediated BCR signaling is a …
The novel Bruton's tyrosine kinase inhibitor ACP-196 shows in vivo efficacy against human chronic lymphocytic leukemia cells xenografted to the NSG mouse model
…, A Montraveta, SEM Herman, T Ingallinera… - Cancer Research, 2014 - AACR
Background: Targeting Bruton's tyrosine kinase (BTK), an essential kinase in the B cell
receptor (BCR) pathway in patients with chronic lymphocytic leukemia (CLL) has proven very …
receptor (BCR) pathway in patients with chronic lymphocytic leukemia (CLL) has proven very …
NX-2127: A first-in-class clinical stage degrader of BTK and IKZF1/3 for the treatment of patients with B cell malignancies
JT Mihalic, N Brathaban, B Bravo, T Ingallinera, D Kato… - Cancer Research, 2023 - AACR
Chronic activation of Bruton’s Tyrosine Kinase (BTK) signaling is a hallmark of B cell malignancies.
Over the last decade, covalent and reversible inhibitors of BTK have proven effective …
Over the last decade, covalent and reversible inhibitors of BTK have proven effective …
[HTML][HTML] CYP3A-mediated drug interaction profile of Bruton tyrosine kinase inhibitor, acalabrutinib
…, T Podoll, M Andrew, CM Krejsa, T Ingallinera… - Blood, 2017 - Elsevier
Background: Acalabrutinib (ACP-196) is a highly selective, potent, covalent inhibitor of
Bruton tyrosine kinase (BTK), in development for the treatment of hematologic malignancies. …
Bruton tyrosine kinase (BTK), in development for the treatment of hematologic malignancies. …