Tositumomab

Summary

Tositumomab (CHEMBL1201604) is an approved antibody targeting MS4A1; indicated across 7 conditions including non-hodgkin lymphoma and lymphoma.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Antibody
• Targets: 1 (MS4A1)
• Indications: 7 conditions
• Clinical trials: 21

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1201604
Name	Tositumomab
Type	Antibody
Max phase	4

Also known as: Tositumomab, Tositumomab component of bexxar, TOSITUMOMAB

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
MS4A1	CD20 (membrane-spanning 4-domains, subfamily A, member 1)	Binding		0%	P11836

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

Target pathways

Aggregated over 1 target gene(s): MS4A1.

Dominant GO biological processes

GO term	Targets
store-operated calcium entry	1
humoral immune response	1
cell surface receptor signaling pathway	1
response to bacterium	1
B cell differentiation	1
B cell proliferation	1
B cell activation	1
B cell receptor signaling pathway	1
protein tetramerization	1
calcium ion import into cytosol	1
positive regulation of calcium ion import across plasma membrane	1

Indications & clinical

Indications

7 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)	Phase	MONDO	EFO
non-Hodgkin lymphoma	3	MONDO:0018908	EFO:0005952
lymphoma	3	MONDO:0005062	EFO:0000574
neoplasm of mature B-cells	2	MONDO:0004949	EFO:0000096
mantle cell lymphoma	2	MONDO:0018876	EFO:1001469
B-cell chronic lymphocytic leukemia	2	MONDO:0004948	EFO:0000095
follicular lymphoma	2	MONDO:0018906	MONDO:0018906
lymphoid leukemia	2	MONDO:0005402	EFO:0004289

Clinical trials

Total trials: 21.

Phase distribution

Phase	Trials
PHASE2	17
PHASE3	3
PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00004874	PHASE3	TERMINATED	Monoclonal Antibody Therapy in Treating Patients With Non-Hodgkin’s Lymphoma
NCT00006721	PHASE3	COMPLETED	S0016 Combination Chemotherapy With Monoclonal Antibody Therapy in Newly Diagnosed Non-Hodgkin’s Lymphoma
NCT00268983	PHASE3	COMPLETED	Comparison Of Rituximab Versus Tositumomab and Iodine I 131 Tositumomab (BEXXAR® Therapeutic Regimen) For Patients With Relapsed Follicular Non-Hodgkins Lymphoma
NCT00003784	PHASE2	COMPLETED	S9911, Combination Chemotherapy Plus Monoclonal Antibody Therapy in Treating Patients With Non-Hodgkin’s Lymphoma
NCT00006695	PHASE2	COMPLETED	Monoclonal Antibody Therapy, Combination Chemotherapy, and Peripheral Stem Cell Transplant in Non-Hodgkin’s Lymphoma
NCT00073931	PHASE2	COMPLETED	Iodine I 131 Tositumomab Followed by Autologous Stem Cell Transplantation in Treating Older Patients With Relapsed or Refractory Non-Hodgkin’s Lymphoma
NCT00107380	PHASE2	COMPLETED	S0433 Iodine I 131 Tositumomab, Rituximab, and Combination Chemotherapy in Treating Older Patients With Stage II, Stage III, or Stage IV Non-Hodgkin’s Lymphoma
NCT00240565	PHASE2	COMPLETED	Tositumomab And Iodine I 131-Tositumomab In Patients With Relapsed Indolent Non-Hodgkin’s Lymphoma
NCT00476047	PHASE2	COMPLETED	Tositumomab and Iodine I 131 Tositumomab in Treating Patients With Chronic Lymphocytic Leukemia or Small Lymphocytic Lymphoma in First Remission
NCT00479167	PHASE2	TERMINATED	A Phase II Trial of Combined Weekly Bortezomib and Tositumomab I-131 in Patients With Relapsed or Refractory Follicular Non-Hodgkin’s Lymphoma
NCT00577629	PHASE2	COMPLETED	Chemotherapy With Monoclonal Antibody and Radioimmunotherapy for High-Risk B-Cell Non-Hodgkins Lymphoma
NCT00770224	PHASE2	COMPLETED	S0801 Iodine I 131 Tositumomab, Rituximab, and Combination Chemotherapy in Previously Untreated Stage II, Stage III, or Stage IV Follicular Non-Hodgkin Lymphoma
NCT00933335	PHASE2	COMPLETED	Study of Safety and Efficacy of a Sequential Regimen Consisting of Three Cycles of Fludarabine Followed by Tositumomab and Iodine I 131 Tositumomab
NCT00938041	PHASE2	COMPLETED	Retreatment of Patients With Non-Hodgkin’s Lymphoma Who Have Previously Responded to Iodine-131 Anti B1 Antibody
NCT00950755	PHASE2	COMPLETED	Study of Iodine 131 Anti B1 Antibody for 1st or 2nd Relapsed Indolent B-Cell Lymphomas or B-Cell Lymphomas That Have Transformed to a More Aggressive Histology
NCT00989664	PHASE2	COMPLETED	Pivotal Study of Iodine I 131 Tositumomab for Chemotherapy-refractory Low-grade or Transformed Low-grade B-cell Non-Hodgkin’s Lymphoma
NCT00992992	PHASE2	COMPLETED	Safety and Efficacy Study of Iodine-131 Anti-B1 Antibody Plus CHOP For Untreated Mantle Cell Lymphoma
NCT00996996	PHASE2	COMPLETED	Iodine-131 Anti-B1 Antibody (Tositumomab and Iodine I 131 Tositumomab) for Previously Untreated, Advanced-stage, Low Grade Non-Hodgkin’s Lymphoma
NCT01224821	PHASE2	COMPLETED	Dosimetry/Validation Study of 131Iodine-Anti B1 (Murine) Radioimmunotherapy for Chemotherapy Refractory Low Grade B Cell Lymphomas and Low Grade Lymphomas That Have Transformed to Higher Grade Histologies
NCT01868035	PHASE2	COMPLETED	Iodine-131 Anti-B1 Antibody Consolidation for Patients With Non-Hodgkin’s Lymphoma Following First-line CHOP
NCT00777114	PHASE1	COMPLETED	Phase 1 Study of Radiosensitization Using Bortezomib in Relapsed Non-Hodgkin’s Lymphoma Patients Receiving Radioimmunotherapy

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).