General
Preferred name
PIRTOBRUTINIB
Synonyms
LOXO-305 ()
LY-3527727 ()
LY3527727 ()
RXC-005 ()
Pirtobrutinib (LOXO-305) ()
LY 3527727, RXC-005 ()
Jaypirca ()
P&D ID
PD154967
CAS
2101700-15-4
Tags
available
drug
Approved by
FDA
First approval
2023
Drug indication
Small lymphocytic lymphoma
Chronic lymphocytic leukaemia
Drug Status
approved
investigational
Max Phase
4.0
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
Pirtobrutinib (LOXO-305, MCL-133) is a selective and reversible (non-covalent), oral Bruton's tyrosine kinase (BTK) inhibitor that was originally developed by LOXO oncology (now Lilly Oncology) for potential to treat B cell malignancies . It binds within the BTK kinase pocket but its interaction does not rely on the C481 residue that is essential for the activity of earlier irreversible BTK inhibitors (, , and ). Therefore, it is expected to be active in cancers with wild type BTK or with C481 resistance mutations.
(GtoPdb)
DESCRIPTION
On January 2023, FDA approved Pirtobrutinib to treat relapsed or refractory mantle cell lymphoma in adults who have had at least two lines of systemic therapy, including a BTK inhibitor
(PKIDB)
DESCRIPTION
Pirtobrutinib is a Bruton's tyrosine kinase (BTK) inhibitor and antineoplastic agent.
(BOC Sciences Bioactive Compounds)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
13
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Approved Drugs
ChEMBL Drugs
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
Guide to Pharmacology
MedChem Express Bioactive Compound Library
PKIDB
Selleckchem Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
15
Molecular Weight
479.16
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
3
Rotatable Bonds
7
Ring Count
3
Aromatic Ring Count
3
cLogP
3.43
TPSA
125.26
Fraction CSP3
0.23
Chiral centers
1.0
Largest ring
6.0
QED
0.45
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Pathway
Protein Tyrosine Kinase/RTK
Target
BTK
Solubility
Soluble in DMSO
Source data