Ibrutinib

Summary

Ibrutinib (CHEMBL1873475) is an approved small-molecule EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor (ATC L01EL01) targeting EGFR, ERBB4, and BLK; indicated across 49 conditions including neoplasm and b-cell chronic lymphocytic leukemia; with CIViC clinical evidence for 10 variant-indication associations (e.g. MYD88 L265P in lymphoplasmacytic lymphoma).

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: L01EL01
• Targets: 16 (EGFR, ERBB4, BLK…)
• Indications: 49 conditions
• Clinical trials: 328
• Precision-oncology evidence (CIViC): 10 variant–indication associations
• Chemistry: 440.5 Da · C25H24N6O2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1873475
Name	Ibrutinib
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	24821094
ChEBI	CHEBI:76612
ATC	L01EL01
Molecular formula	C25H24N6O2
Molecular weight	440.5
InChIKey	XYFPWWZEPKGCCK-GOSISDBHSA-N

SMILES: C=CC(=O)N1CCC[C@H](C1)N2C3=NC=NC(=C3C(=N2)C4=CC=C(C=C4)OC5=CC=CC=C5)N

IUPAC name: 1-[(3R)-3-[4-amino-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]prop-2-en-1-one

ChEBI definition: A member of the class of acrylamides that is (3R)-3-[4-amino-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine in which the piperidine nitrogen is replaced by an acryloyl group. A selective and covalent inhibitor of the enzyme Bruton’s tyrosine kinase, it is used for treatment of B-cell malignancies.

Pharmacological roles (ChEBI): EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor, antineoplastic agent.

Also known as: CRA-032765, Ibrutinib, Imbruvica, PC-32765, PCI 32765, PCI-32765, IBRUTINIB, IMBRUVICA, SID124898784, SID174007139, ibrutinib, Iibrutinib

Patent coverage: 3,199 distinct patent families (7,994 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
EGFR	epidermal growth factor receptor	Inhibition	8.28	17.5%	P00533
ERBB4	erb-b2 receptor tyrosine kinase 4	Inhibition	8.47	0.7%	Q15303
BLK	BLK proto-oncogene, Src family tyrosine kinase	Inhibition	10	0.1%	P51451
BMX	BMX non-receptor tyrosine kinase	Inhibition	9.1	0%	P51813
BTK	Bruton tyrosine kinase	Inhibition	8.82	0.7%	Q06187
ERBB2	erb-b2 receptor tyrosine kinase 2	Inhibition	8.19	17.7%	P04626
FYN	FYN proto-oncogene, Src family tyrosine kinase	Inhibition	7.54	0%	P06241
HCK	HCK proto-oncogene, Src family tyrosine kinase	Inhibition	7.54	0.1%	P08631
ITK	IL2 inducible T cell kinase	Inhibition	8.31	0%	Q08881
JAK3	Janus kinase 3	Inhibition	7.49	0.6%	P52333
LCK	LCK proto-oncogene, Src family tyrosine kinase	Inhibition	8.2	0.1%	P06239
LYN	LYN proto-oncogene, Src family tyrosine kinase	Inhibition	7.7	0.5%	P07948
SRC	SRC proto-oncogene, non-receptor tyrosine kinase	Inhibition	7.72	3.7%	P12931
TEC	tec protein tyrosine kinase	Inhibition	8.15	0.1%	P42680
TXK	TXK tyrosine kinase	Inhibition	8.7	0.7%	P42681
YES1	YES proto-oncogene 1, Src family tyrosine kinase	Inhibition	8.39	0.7%	P07947

Broader ChEMBL bioactivity targets: 59 (assay-derived). Sample: Receptor-interacting serine/threonine-protein kinase 3, Receptor tyrosine-protein kinase erbB-2, Tyrosine-protein kinase Fyn, Macrophage colony-stimulating factor 1 receptor, Tyrosine-protein kinase ABL1, Nuclear receptor subfamily 4 group A member 3, Receptor-type tyrosine-protein kinase FLT3, Epidermal growth factor receptor, Proto-oncogene tyrosine-protein kinase receptor Ret, Thromboxane A2 receptor.

Bioactivity

ChEMBL activities: 443 potent at pChembl ≥ 5 of 465 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
BTK	10.1	IC50	0.08	nM	CHEMBL_ACT_20654540
ERBB4	10	IC50	0.1	nM	CHEMBL_ACT_17719998
ERBB4	10	IC50	0.1	nM	CHEMBL_ACT_17758421
BTK	10	IC50	0.1	nM	CHEMBL_ACT_19173518
BLK	10	IC50	0.1	nM	CHEMBL_ACT_22877477
BLK	10	IC50	0.1	nM	CHEMBL_ACT_24773304
BLK	10	IC50	0.1	nM	CHEMBL_ACT_25091631
BTK	10	IC50	0.1	nM	CHEMBL_ACT_26016653
BLK	10	IC50	0.1	nM	CHEMBL_ACT_26315223
ERBB4	10	IC50	0.1	nM	CHEMBL_ACT_26609827
ERBB4	10	IC50	0.1	nM	CHEMBL_ACT_26622311
BTK	9.96	IC50	0.11	nM	CHEMBL_ACT_18092352
BTK	9.74	IC50	0.18	nM	CHEMBL_ACT_29257915
BTK	9.7	IC50	0.2	nM	CHEMBL_ACT_18679229
BTK	9.7	IC50	0.2	nM	CHEMBL_ACT_18752978
BTK	9.7	IC50	0.2	nM	CHEMBL_ACT_24693327
BTK	9.68	IC50	0.21	nM	CHEMBL_ACT_18934900
BTK	9.68	IC50	0.21	nM	CHEMBL_ACT_28147304
BLK	9.64	IC50	0.23	nM	CHEMBL_ACT_19306061
BTK	9.62	Ki	0.24	nM	CHEMBL_ACT_25927538
ERBB4	9.6	IC50	0.25	nM	CHEMBL_ACT_19306067
BTK	9.52	IC50	0.3	nM	CHEMBL_ACT_16772254
BTK	9.52	IC50	0.3	nM	CHEMBL_ACT_18687152
BTK	9.52	IC50	0.3	nM	CHEMBL_ACT_20631322
BTK	9.48	IC50	0.33	nM	CHEMBL_ACT_18562712
BTK	9.47	IC50	0.34	nM	CHEMBL_ACT_16828854
BTK	9.47	IC50	0.34	nM	CHEMBL_ACT_17952362
BTK	9.47	IC50	0.34	nM	CHEMBL_ACT_18248762
BTK	9.4	IC50	0.4	nM	CHEMBL_ACT_18502847
BTK	9.4	IC50	0.4	nM	CHEMBL_ACT_18666975

Target pathways

Aggregated over 16 target gene(s): EGFR, ERBB4, BLK, BMX, BTK, ERBB2, FYN, HCK, ITK, JAK3, LCK, LYN, SRC, TEC, TXK, YES1.

Top Reactome pathways

277 total, by targets touching each:

Pathway	Targets	Genes
Immune System	8	BLK, BTK, ITK, JAK3, LCK, LYN, SRC, TEC
Signaling by ERBB2	6	EGFR, ERBB2, ERBB4, FYN, SRC, YES1
PIP3 activates AKT signaling	6	EGFR, ERBB2, ERBB4, FYN, LCK, SRC
Signaling by SCF-KIT	6	FYN, LCK, LYN, SRC, TEC, YES1
Signal Transduction	6	BTK, JAK3, LCK, LYN, SRC, TEC
Constitutive Signaling by Aberrant PI3K in Cancer	6	EGFR, ERBB2, ERBB4, FYN, LCK, SRC
RAF/MAP kinase cascade	6	EGFR, ERBB2, ERBB4, FYN, JAK3, SRC
PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling	6	EGFR, ERBB2, ERBB4, FYN, LCK, SRC
FCGR3A-mediated phagocytosis	6	BTK, FYN, HCK, LYN, SRC, YES1
Cytokine Signaling in Immune system	5	JAK3, LCK, LYN, SRC, TEC
Adaptive Immune System	5	BLK, BTK, ITK, LCK, LYN
Regulation of KIT signaling	5	FYN, LCK, LYN, SRC, YES1
Disease	5	BTK, JAK3, LCK, LYN, SRC
Innate Immune System	5	BTK, ITK, LCK, LYN, TEC
FCGR activation	5	FYN, HCK, LYN, SRC, YES1
PECAM1 interactions	5	FYN, LCK, LYN, SRC, YES1
FCERI mediated Ca+2 mobilization	5	BTK, ITK, LYN, TEC, TXK
Co-stimulation by CD28	5	FYN, LCK, LYN, SRC, YES1
Co-inhibition by CTLA4	5	FYN, LCK, LYN, SRC, YES1
Infectious disease	5	BTK, JAK3, LCK, LYN, SRC
Signaling by Receptor Tyrosine Kinases	5	JAK3, LCK, LYN, SRC, TEC
FCGR3A-mediated IL10 synthesis	5	FYN, HCK, LYN, SRC, YES1
Signaling by phosphorylated juxtamembrane, extracellular and kinase domain KIT mutants	5	FYN, LCK, LYN, SRC, YES1
Signaling by CSF1 (M-CSF) in myeloid cells	5	FYN, HCK, LYN, SRC, YES1
Fc epsilon receptor (FCERI) signaling	4	BTK, ITK, LYN, TEC
EPH-Ephrin signaling	4	FYN, LYN, SRC, YES1
EPHB-mediated forward signaling	4	FYN, LYN, SRC, YES1
EPHA-mediated growth cone collapse	4	FYN, LYN, SRC, YES1
EPH-ephrin mediated repulsion of cells	4	FYN, LYN, SRC, YES1
Signaling by Interleukins	4	JAK3, LCK, LYN, TEC

Dominant GO biological processes

GO term	Targets
protein phosphorylation	16
intracellular signal transduction	12
cell surface receptor protein tyrosine kinase signaling pathway	9
peptidyl-tyrosine phosphorylation	9
immune system process	9
adaptive immune response	8
signal transduction	7
B cell receptor signaling pathway	7
protein autophosphorylation	6
cell differentiation	6
T cell receptor signaling pathway	6
leukocyte migration	6
cell surface receptor signaling pathway	5
negative regulation of apoptotic process	5
positive regulation of MAPK cascade	5

Indications & clinical

Indications

49 indications (6 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
neoplasm	4	MONDO:0005070	EFO:0000616
B-cell chronic lymphocytic leukemia	4	MONDO:0004948	EFO:0000095
mantle cell lymphoma	4	MONDO:0018876	EFO:1001469
Waldenstrom macroglobulinemia	4	MONDO:0100280	EFO:0009441
lymphoma	3	MONDO:0005062	EFO:0000574
neoplasm of mature B-cells	3	MONDO:0004949	EFO:0000096
non-Hodgkin lymphoma	3	MONDO:0018908	EFO:0005952
diffuse large B-cell lymphoma	3	MONDO:0018905	EFO:0000403
marginal zone lymphoma	3	MONDO:0017604	EFO:1000630
graft versus host disease	3	MONDO:0013730	MONDO:0013730
follicular lymphoma	3	MONDO:0018906	MONDO:0018906
plasma cell myeloma	2	MONDO:0009693	EFO:0001378
leukemia	2	MONDO:0005059	EFO:0000565
lymphoid leukemia	2	MONDO:0005402	EFO:0004289
acute myeloid leukemia	2	MONDO:0018874	EFO:0000222
Hodgkins lymphoma	2	MONDO:0004952	EFO:0000183
carcinoid tumor	2	MONDO:0005369	EFO:0004243
Burkitt lymphoma	2	MONDO:0007243	EFO:0000309
cutaneous melanoma	2	MONDO:0005012	EFO:0000389
metastatic melanoma	2	MONDO:0005191	EFO:0002617
non-small cell lung carcinoma	2	MONDO:0005233	EFO:0003060
amyloidosis	2	MONDO:0019065	EFO:1001875
food allergy	2	MONDO:0700226	EFO:1001890
autoimmune hemolytic anemia	2	MONDO:0020108	EFO:1001264
head and neck squamous cell carcinoma	2	MONDO:0010150	EFO:0000181
mast cell leukemia	2	MONDO:0020334	EFO:0007359
T-cell prolymphocytic leukemia	2	MONDO:0019468	EFO:1000560
prolymphocytic leukemia	2	MONDO:0001023	MONDO:0001023
hematopoietic and lymphoid system neoplasm	2	MONDO:0002334	MONDO:0044881
severe acute respiratory syndrome	2	MONDO:0005091	MONDO:0100096
anaphylaxis	2	MONDO:0100053	MONDO:0100053
lymphoid neoplasm	2	MONDO:0005157	EFO:0001642
head and neck cancer	2	MONDO:0005627	EFO:0006859
liver disorder	1	MONDO:0005154	EFO:0001421
acute lymphoblastic leukemia	1	MONDO:0004967	EFO:0000220
myelodysplastic syndrome	1	MONDO:0018881	EFO:0000198
renal cell carcinoma	1	MONDO:0005086	EFO:0000681
glioblastoma	1	MONDO:0018177	EFO:0000519
breast neoplasm	1	MONDO:0021100	MONDO:0007254
lung neoplasm	1	MONDO:0021117	MONDO:0008903
colonic neoplasm	1	MONDO:0005401	MONDO:0021063
colorectal neoplasm	1	MONDO:0005335	MONDO:0005575

7 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 328.

Phase distribution

Phase	Trials
PHASE2	142
PHASE1	71
PHASE1/PHASE2	53
PHASE3	42
Not specified	12
PHASE4	3
PHASE2/PHASE3	3
EARLY_PHASE1	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT03229200	PHASE4	ACTIVE_NOT_RECRUITING	Extended Treatment Protocol for Subjects Continuing to Benefit From Ibrutinib.
NCT03190330	PHASE4	COMPLETED	A Study to Assess Safety of ImbruvicaTM in Indian Participants With Chronic Lymphocytic Leukemia or Mantle Cell Lymphoma Who Have Received at Least One Prior Therapy or Chronic Lymphocytic Leukemia With 17p Deletion
NCT04042376	PHASE4	COMPLETED	A Study of Ibrutinib (PCI-32765) in Chinese Participants With Relapse or Refractory Waldenstrom’s Macroglobulinemia (WM)
NCT01804686	PHASE3	RECRUITING	A Long-term Extension Study of PCI-32765 (Ibrutinib)
NCT01886872	PHASE3	ACTIVE_NOT_RECRUITING	Rituximab and Bendamustine Hydrochloride, Rituximab and Ibrutinib, or Ibrutinib Alone in Treating Older Patients With Previously Untreated Chronic Lymphocytic Leukemia
NCT02048813	PHASE3	ACTIVE_NOT_RECRUITING	Ibrutinib and Rituximab Compared With Fludarabine Phosphate, Cyclophosphamide, and Rituximab in Treating Patients With Untreated Chronic Lymphocytic Leukemia or Small Lymphocytic Lymphoma
NCT02443077	PHASE3	ACTIVE_NOT_RECRUITING	Ibrutinib Before and After Stem Cell Transplant in Treating Patients With Relapsed or Refractory Diffuse Large B-cell Lymphoma
NCT02477696	PHASE3	ACTIVE_NOT_RECRUITING	Study of Acalabrutinib (ACP-196) Versus Ibrutinib in Previously Treated Participants With High Risk Chronic Lymphocytic Leukemia (CLL)
NCT02858258	PHASE3	RECRUITING	ASCT After a Rituximab/Ibrutinib/Ara-c Containing iNduction in Generalized Mantle Cell Lymphoma
NCT03462719	PHASE3	ACTIVE_NOT_RECRUITING	A Study of the Combination of Ibrutinib Plus Venetoclax Versus Chlorambucil Plus Obinutuzumab for the First-line Treatment of Participants With Chronic Lymphocytic Leukemia (CLL)/Small Lymphocytic Lymphoma (SLL)
NCT03701282	PHASE3	ACTIVE_NOT_RECRUITING	Assessing the Ability of Combination Treatment With Venetoclax to Permit Time Limited Therapy in Chronic Lymphocytic Leukemia
NCT03737981	PHASE3	ACTIVE_NOT_RECRUITING	Testing the Addition of a New Anti-cancer Drug, Venetoclax, to the Usual Treatment (Ibrutinib and Obinutuzumab) in Untreated, Older Patients With Chronic Lymphocytic Leukemia
NCT04061512	PHASE2/PHASE3	RECRUITING	Rituximab and Ibrutinib (RI) Versus Dexamethasone, Rituximab and Cyclophosphamide (DRC) as Initial Therapy for Waldenström’s Macroglobulinaemia
NCT04212013	PHASE3	ACTIVE_NOT_RECRUITING	A Study of Ibrutinib With Rituximab in People With Untreated Marginal Zone Lymphoma
NCT04608318	PHASE3	ACTIVE_NOT_RECRUITING	Ibrutinib Monotherapy Versus Fixed-duration Venetoclax Plus Obinutuzumab Versus Fixed-duration Ibrutinib Plus Venetoclax in Patients With Previously Untreated Chronic Lymphocytic Leukaemia (CLL)
NCT04662255	PHASE3	ACTIVE_NOT_RECRUITING	Study of BTK Inhibitor LOXO-305 Versus Approved BTK Inhibitor Drugs in Patients With Mantle Cell Lymphoma (MCL)
NCT05254743	PHASE3	RECRUITING	A Study of Pirtobrutinib (LOXO-305) Versus Ibrutinib in Participants With Chronic Lymphocytic Leukemia (CLL)/Small Lymphocytic Lymphoma (SLL)
NCT06136559	PHASE3	RECRUITING	A Study of Nemtabrutinib (MK-1026) Versus Comparator (Investigator’s Choice of Ibrutinib or Acalabrutinib) in First Line (1L) Chronic Lymphocytic Leukemia (CLL)/ Small Lymphocytic Lymphoma (SLL) (MK-1026-011/BELLWAVE-011)
NCT07377578	PHASE3	RECRUITING	A Study of Rocbrutinib Versus Investigator’s Choice of BTK Inhibitors in Patients With Relapsed or Refractory Mantle Cell Lymphoma
NCT01578707	PHASE3	COMPLETED	A Phase 3 Study of Ibrutinib (PCI-32765) Versus Ofatumumab in Patients With Relapsed or Refractory Chronic Lymphocytic Leukemia
NCT01611090	PHASE3	COMPLETED	A Study of Ibrutinib in Combination With Bendamustine and Rituximab in Patients With Relapsed or Refractory Chronic Lymphocytic Leukemia or Small Lymphocytic Lymphoma
NCT01646021	PHASE3	COMPLETED	Study of Ibrutinib (a Bruton’s Tyrosine Kinase Inhibitor), Versus Temsirolimus in Patients With Relapsed or Refractory Mantle Cell Lymphoma Who Have Received at Least One Prior Therapy
NCT01722487	PHASE3	COMPLETED	Open-label Phase 3 BTK Inhibitor Ibrutinib vs Chlorambucil Patients 65 Years or Older With Treatment-naive CLL or SLL
NCT01724346	PHASE3	COMPLETED	Open-label Extension Study in Patients 65 Years or Older With Chronic Lymphocytic Leukemia or Small Lymphocytic Lymphoma
NCT01776840	PHASE3	COMPLETED	A Study of the Bruton’s Tyrosine Kinase Inhibitor Ibrutinib Given in Combination With Bendamustine and Rituximab in Patients With Newly Diagnosed Mantle Cell Lymphoma
NCT01855750	PHASE3	COMPLETED	A Study of the Bruton’s Tyrosine Kinase Inhibitor, PCI-32765 (Ibrutinib), in Combination With Rituximab, Cyclophosphamide, Doxorubicin, Vincristine, and Prednisone in Patients With Newly Diagnosed Non-Germinal Center B-Cell Subtype of Diffuse Large B-Cell Lymphoma
NCT01973387	PHASE3	COMPLETED	A Study of PCI-32765 (Ibrutinib) Versus Rituximab in Relapsed or Refractory Chronic Leukemia/Lymphoma
NCT01974440	PHASE3	COMPLETED	A Study of PCI-32765 (Ibrutinib) in Combination With Either Bendamustine and Rituximab or Rituximab, Cyclophosphamide, Doxorubicin, Vincristine, and Prednisone in Participants With Previously Treated Indolent Non-Hodgkin Lymphoma
NCT02165397	PHASE3	COMPLETED	Ibrutinib With Rituximab in Adults With Waldenström’s Macroglobulinemia
NCT02264574	PHASE3	COMPLETED	A Multi-Center Study of Ibrutinib in Combination With Obinutuzumab Versus Chlorambucil in Combination With Obinutuzumab in Patients With Treatment naïve Chronic Lymphocytic Leukemia (CLL) or Small Lymphocytic Lymphoma (SLL)
NCT02301156	PHASE3	COMPLETED	Ublituximab in Combination With Ibrutinib Versus Ibrutinib Alone in Participants With Previously Treated High-Risk Chronic Lymphocytic Leukemia (CLL)
NCT02436668	PHASE3	COMPLETED	Study of Ibrutinib vs Placebo, in Combination With Nab-paclitaxel and Gemcitabine, in the First Line Treatment of Patients With Metastatic Pancreatic Adenocarcinoma (RESOLVE)
NCT02703272	PHASE3	TERMINATED	A Safety and Efficacy Study of Ibrutinib in Pediatric and Young Adult Participants With Relapsed or Refractory Mature B-cell Non-Hodgkin Lymphoma
NCT02735876	PHASE3	WITHDRAWN	A Study of Acalabrutinib in Combination With Rituximab Versus Ibrutinib Versus Acalabrutinib in Subjects With Relapsed or Refractory Mantle Cell Lymphoma
NCT02757040	PHASE3	UNKNOWN	Combination of Ibrutinib and As2O3 in the Treatment of CLL
NCT02801578	PHASE2/PHASE3	COMPLETED	A Study of Different Doses of Ibrutinib in Participants With Chronic Lymphocytic Leukemia (CLL)
NCT02863718	PHASE3	COMPLETED	Ibrutinib in Previously Untreated Binet Stage A Chronic Lymphocytic Leukemia With Risk of Disease Progression
NCT02947347	PHASE3	COMPLETED	Study of Ibrutinib and Rituximab in Treatment Naïve Follicular Lymphoma
NCT02950051	PHASE3	COMPLETED	Standard Chemoimmunotherapy (FCR/BR) Versus Rituximab + Venetoclax (RVe) Versus Obinutuzumab (GA101) + Venetoclax (GVe) Versus Obinutuzumab + Ibrutinib + Venetoclax (GIVe) in Fit Patients With Previously Untreated Chronic Lymphocytic Leukemia (CLL) Without Del(17p) or TP53 Mutation
NCT02959944	PHASE3	COMPLETED	Ibrutinib in Combination With Corticosteroids vs Placebo in Combination With Corticosteroids in Participants With New Onset Chronic Graft Versus Host Disease (cGVHD)

Clinical evidence (CIViC)

Variant × indication × effect (10 predictive associations from 11 curated evidence items):

Variant	Indication	Effect	Therapy	Level	CIViC
MYD88 L265P	Lymphoplasmacytic Lymphoma	Sensitivity/Response	Ibrutinib	CIViC B	EID986
BTK C481S	Chronic Lymphocytic Leukemia	Resistance	Ibrutinib	CIViC B	EID1770 +1
BTK T316A	Chronic Lymphocytic Leukemia	Resistance	Ibrutinib	CIViC C	EID1985
BLK Expression	B-cell Acute Lymphoblastic Leukemia	Sensitivity/Response	Ibrutinib	CIViC D	EID9288
BTK Expression	B-cell Acute Lymphoblastic Leukemia	Sensitivity/Response	Ibrutinib	CIViC D	EID9287
ERBB2 Amplification	Esophageal Cancer	Sensitivity/Response	Ibrutinib	CIViC D	EID6929
MYC Amplification	Esophageal Carcinoma	Sensitivity/Response	Ibrutinib	CIViC D	EID6928
PIM1 L2V	Diffuse Large B-cell Lymphoma Activated B-cell Type	Resistance	Ibrutinib	CIViC D	EID9945
PIM1 P81S	Diffuse Large B-cell Lymphoma Activated B-cell Type	Resistance	Ibrutinib	CIViC D	EID9946
PIM1 S97N	Diffuse Large B-cell Lymphoma Activated B-cell Type	Resistance	Ibrutinib	CIViC D	EID9947

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 0 clinical and 8 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

317 molecules share ≥1 primary target. Top 60 by shared-target count:

Molecule	Source	Status	Shared targets
AFATINIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BMX, BTK, EGFR, ERBB2, ERBB4, FYN, HCK, ITK, JAK3, LCK, LYN, SRC, TEC, TXK, YES1
BOSUTINIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BMX, BTK, EGFR, ERBB2, ERBB4, FYN, HCK, ITK, JAK3, LCK, LYN, SRC, TEC, TXK, YES1
CRIZOTINIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BMX, BTK, EGFR, ERBB2, ERBB4, FYN, HCK, ITK, JAK3, LCK, LYN, SRC, TEC, TXK, YES1
Pazopanib	ChEMBL + PubChem	Phase 4 (approved)	BLK, BMX, BTK, EGFR, ERBB2, ERBB4, FYN, HCK, ITK, JAK3, LCK, LYN, SRC, TEC, TXK, YES1
SELUMETINIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BMX, BTK, EGFR, ERBB2, ERBB4, FYN, HCK, ITK, JAK3, LCK, LYN, SRC, TEC, TXK, YES1
DASATINIB	ChEMBL	Phase 4 (approved)	BLK, BMX, BTK, EGFR, ERBB2, ERBB4, FYN, HCK, ITK, JAK3, LCK, LYN, SRC, TEC, TXK, YES1
CANERTINIB	ChEMBL	Phase 3	BLK, BMX, BTK, EGFR, ERBB2, ERBB4, FYN, HCK, ITK, JAK3, LCK, LYN, SRC, TEC, TXK, YES1
R-406	ChEMBL	Phase 2	BLK, BMX, BTK, EGFR, ERBB2, ERBB4, FYN, HCK, ITK, JAK3, LCK, LYN, SRC, TEC, TXK, YES1
FEDRATINIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BMX, BTK, EGFR, ERBB4, FYN, HCK, ITK, JAK3, LCK, LYN, SRC, TEC, TXK, YES1
GEFITINIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BMX, EGFR, ERBB2, ERBB4, FYN, HCK, ITK, JAK3, LCK, LYN, SRC, TEC, TXK, YES1
ZANUBRUTINIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BMX, BTK, EGFR, ERBB2, ERBB4, FYN, HCK, ITK, JAK3, LCK, LYN, TEC, TXK, YES1
LESTAURTINIB	ChEMBL	Phase 3	BLK, BMX, BTK, EGFR, ERBB4, FYN, HCK, ITK, JAK3, LCK, LYN, SRC, TEC, TXK, YES1
FORETINIB	ChEMBL	Phase 2	BLK, BMX, BTK, EGFR, ERBB2, ERBB4, FYN, HCK, ITK, LCK, LYN, SRC, TEC, TXK, YES1
PELITINIB	ChEMBL	Phase 2	BLK, BMX, BTK, EGFR, ERBB2, ERBB4, FYN, HCK, ITK, JAK3, LCK, LYN, SRC, TXK, YES1
Idelalisib	PubChem	Approved	BLK, BMX, BTK, ERBB2, ERBB4, FYN, HCK, ITK, JAK3, LCK, LYN, SRC, TEC, TXK, YES1
ERLOTINIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BMX, EGFR, ERBB2, ERBB4, FYN, HCK, JAK3, LCK, LYN, SRC, TEC, TXK, YES1
SUNITINIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BMX, BTK, EGFR, FYN, HCK, ITK, JAK3, LCK, LYN, SRC, TEC, TXK, YES1
VANDETANIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BMX, BTK, EGFR, ERBB2, ERBB4, FYN, HCK, LCK, LYN, SRC, TEC, TXK, YES1
TOZASERTIB	ChEMBL	Phase 2	BLK, BMX, BTK, EGFR, FYN, HCK, ITK, JAK3, LCK, LYN, SRC, TEC, TXK, YES1
BRIGATINIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BTK, EGFR, ERBB2, ERBB4, FYN, HCK, LCK, LYN, SRC, TEC, TXK, YES1
NERATINIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BTK, EGFR, ERBB2, ERBB4, FYN, HCK, JAK3, LCK, LYN, SRC, TXK, YES1
DACOMITINIB	ChEMBL + PubChem	Phase 4 (approved)	BTK, EGFR, ERBB2, ERBB4, FYN, HCK, JAK3, LCK, LYN, SRC, TEC, YES1
SORAFENIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BMX, EGFR, ERBB2, FYN, HCK, JAK3, LCK, LYN, SRC, TEC, TXK
MIDOSTAURIN	ChEMBL + PubChem	Phase 4 (approved)	BLK, EGFR, ERBB4, FYN, HCK, JAK3, LCK, LYN, SRC, TXK, YES1
NINTEDANIB	ChEMBL	Phase 4 (approved)	BLK, BTK, FYN, HCK, ITK, JAK3, LCK, LYN, SRC, TXK, YES1
CEDIRANIB	ChEMBL	Phase 3	BLK, BTK, EGFR, ERBB2, ERBB4, FYN, HCK, LCK, LYN, SRC, YES1
DOVITINIB	ChEMBL	Phase 3	BLK, BTK, EGFR, FYN, HCK, ITK, JAK3, LCK, LYN, SRC, YES1
CENISERTIB	ChEMBL	Phase 2	BLK, BTK, EGFR, ERBB2, ERBB4, FYN, ITK, JAK3, LCK, LYN, SRC
SU-014813	ChEMBL	Phase 2	BLK, BTK, EGFR, FYN, HCK, ITK, JAK3, LCK, LYN, SRC, YES1
ACALABRUTINIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BMX, BTK, EGFR, ERBB2, ERBB4, ITK, JAK3, TEC, TXK
IMATINIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BMX, EGFR, ERBB2, FYN, LCK, LYN, SRC, TEC, TXK
MOBOCERTINIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BMX, BTK, EGFR, ERBB2, ERBB4, ITK, JAK3, TEC, TXK
NILOTINIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BMX, FYN, HCK, LCK, LYN, SRC, TEC, TXK, YES1
PONATINIB	ChEMBL + PubChem	Phase 4 (approved)	BTK, EGFR, ERBB2, FYN, HCK, LCK, LYN, SRC, TEC, YES1
REMIBRUTINIB	ChEMBL	Phase 3	BLK, BMX, BTK, EGFR, ERBB2, ERBB4, ITK, JAK3, TEC, TXK
ILORASERTIB	ChEMBL	Phase 2	BLK, BTK, EGFR, ERBB2, ERBB4, FYN, ITK, LCK, LYN, SRC
REBASTINIB	ChEMBL	Phase 2	BLK, BMX, BTK, FYN, HCK, ITK, LCK, LYN, SRC, YES1
Binimetinib	PubChem	Approved	BTK, EGFR, ERBB2, FYN, HCK, LCK, LYN, SRC, TEC, YES1
AXITINIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BMX, EGFR, ITK, JAK3, LCK, TEC, TXK, YES1
LAPATINIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BMX, EGFR, ERBB2, ERBB4, HCK, SRC, TEC, TXK
QUIZARTINIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BMX, HCK, ITK, LCK, LYN, TEC, TXK, YES1
RITLECITINIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BMX, BTK, ERBB2, ERBB4, ITK, JAK3, TEC, TXK
MASITINIB	ChEMBL	Phase 3	BLK, EGFR, ERBB2, FYN, HCK, LCK, LYN, SRC, YES1
AT-9283	ChEMBL	Phase 2	BTK, FYN, HCK, JAK3, LCK, LYN, SRC, TEC, YES1
ATUZABRUTINIB	ChEMBL	Phase 2	BLK, BMX, BTK, EGFR, ERBB2, ERBB4, ITK, TEC, TXK
DEFOSBARASERTIB	ChEMBL	Phase 2	BLK, BTK, EGFR, ERBB2, ERBB4, HCK, LCK, LYN, YES1
ENTRECTINIB	ChEMBL + PubChem	Phase 4 (approved)	BLK, BTK, FYN, JAK3, LCK, LYN, SRC, TEC
TIRABRUTINIB	ChEMBL	Phase 4 (approved)	BLK, BMX, BTK, ERBB2, ERBB4, LCK, TEC, TXK
ALISERTIB	ChEMBL	Phase 3	BLK, BTK, EGFR, ERBB2, ERBB4, HCK, LCK, SRC
SARACATINIB	ChEMBL	Phase 3	BTK, EGFR, FYN, HCK, LCK, LYN, SRC, YES1
BMS-986142	ChEMBL	Phase 2	BLK, BMX, BTK, ITK, LCK, SRC, TEC, TXK
BRANEBRUTINIB	ChEMBL	Phase 2	BMX, BTK, EGFR, ERBB4, ITK, JAK3, TEC, TXK
DANUSERTIB	ChEMBL	Phase 2	BTK, FYN, HCK, LCK, LYN, SRC, TEC, YES1
DORAMAPIMOD	ChEMBL	Phase 2	BLK, EGFR, FYN, HCK, LCK, LYN, SRC, YES1
OSI-632	ChEMBL	Phase 2	BLK, EGFR, FYN, ITK, LCK, LYN, SRC, YES1
SPEBRUTINIB	ChEMBL	Phase 2	BMX, BTK, EGFR, ITK, JAK3, LYN, TEC, TXK
Fostamatinib	PubChem	Approved	BTK, FYN, HCK, LCK, LYN, SRC, TEC, YES1
regorafenib	PubChem	Approved	BTK, FYN, HCK, LCK, LYN, SRC, TEC, YES1
CABOZANTINIB	ChEMBL + PubChem	Phase 4 (approved)	EGFR, ERBB2, HCK, LCK, LYN, SRC, TEC
CERITINIB	ChEMBL + PubChem	Phase 4 (approved)	BTK, EGFR, JAK3, LCK, LYN, SRC, TEC