Details of the Drug

General Information of Drug (ID: DM295PR)

• Drug Name: Ofatumumab
• Synonyms: Arzerra (TN)

Indication

Disease Entry	ICD 11	Status	REF
Chronic lymphocytic leukaemia	2A82.0	Approved	[1]
Small lymphocytic lymphoma	2A82.0	Approved	[2]
Diffuse large B-cell lymphoma	2A81	Phase 3	[1]
Non-hodgkin lymphoma	2B33.5	Phase 3	[3]
Rheumatoid arthritis	FA20	Phase 2	[1]

• Affected Organisms: Humans and other mammals
• ATC Code:
  L01FA02: Ofatumumab
  L01FA: CD20 (Clusters of Differentiation 20) inhibitors
  L01F: MONOCLONAL ANTIBODIES AND ANTIBODY DRUG CONJUGATES
  L01: ANTINEOPLASTIC AGENTS
  L: ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
  L04AA52: Ofatumumab
  L04AA: Selective immunosuppressants
  L04A: IMMUNOSUPPRESSANTS
  L04: IMMUNOSUPPRESSANTS
  L: ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
• Drug Type: Antibody
• Sequence:
  >heavy chain
  EVQLVESGGGLVQPGRSLRLSCAASGFTFNDYAMHWVRQAPGKGLEWVSTISWNSGSIGY
  ADSVKGRFTISRDNAKKSLYLQMNSLRAEDTALYYCAKDIQYGNYYYGMDVWGQGTTVTV
  SSASTKGPSVFPLAPGSSKSTSGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQ
  SSGLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEP
  >light chain
  EIVLTQSPATLSLSPGERATLSCRASQSVSSYLAWYQQKPGQAPRLLIYDASNRATGIPA
  RFSGSGSGTDFTLTISSLEPEDFAVYYCQQRSNWPITFGQGTRLEIKRTVAAPSVFIFPP
  SDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLT
  LSKADYEKHKVYACEVTHQGLSSPVTKSFNR
• ADMET Property:
  Absorption Cmax: The maximum plasma concentration (Cmax) of drug is 94 mg/L [4]
  Absorption Tmax: The time to maximum plasma concentration (Tmax) is 7.3 h [4]
  Clearance: The clearance of drug is 11.6 mL/h [5]
  Half-life: The concentration or amount of drug in body reduced by one-half in 17.1 days [5]
  Metabolism: The drug is metabolized via the reticuloendothelial system and protein catabolism by a target\mediated disposition pathway [6]
  Vd: The volume of distribution (Vd) of drug is 5.8 L [5]
• Cross-matching ID:
  UNII: M95KG522R0
  DrugBank ID: DB06650
  TTD ID: D0Y8ZN
• Drug-Molecule Activity Atlas (DMA)NEW: Click to Jump to the Detailed DMA Information of This Drug
• Repurposed Drugs (RPD): Click to Jump to the Detailed RPD Information of This Drug

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Leukocyte surface antigen Leu-16 (CD20)	TTUE541	CD20_HUMAN	Not Available	[7]

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Ofatumumab (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Teriflunomide	DMQ2FKJ	Major	Additive myelosuppressive effects by the combination of Ofatumumab and Teriflunomide.	Hyper-lipoproteinaemia [5C80]	[8]
Tecfidera	DM2OVDT	Moderate	Additive immunosuppressive effects by the combination of Ofatumumab and Tecfidera.	Multiple sclerosis [8A40]	[9]
Siponimod	DM2R86O	Major	Additive immunosuppressive effects by the combination of Ofatumumab and Siponimod.	Multiple sclerosis [8A40]	[10]
Fingolimod	DM5JVAN	Major	Additive immunosuppressive effects by the combination of Ofatumumab and Fingolimod.	Multiple sclerosis [8A40]	[11]
Ocrelizumab	DMEZ2KH	Moderate	Additive immunosuppressive effects by the combination of Ofatumumab and Ocrelizumab.	Multiple sclerosis [8A40]	[12]
Ozanimod	DMT6AM2	Major	Additive immunosuppressive effects by the combination of Ofatumumab and Ozanimod.	Multiple sclerosis [8A40]	[13]
Golimumab	DMHZV7X	Major	Additive immunosuppressive effects by the combination of Ofatumumab and Golimumab.	Rheumatoid arthritis [FA20]	[14]
Anthrax vaccine	DM9GSWY	Moderate	Antagonize the effect of Ofatumumab when combined with Anthrax vaccine.	Sepsis [1G40-1G41]	[15]

References

• [1] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6778).
• [2] Final analysis from RESONATE: Up to six years of follow-up on ibrutinib in patients with previously treated chronic lymphocytic leukemia or small lymphocytic lymphoma. Am J Hematol. 2019 Dec;94(12):1353-1363.
• [3] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [4] Ogura M, Hatake K, Tobinai K, Uchida T, Suzuki T, Terui Y, Yokoyama M, Maruyama D, Mori M, Jewell RC, Katsura K, Hotta T: Phase I study of ofatumumab, a human anti-CD20 antibody, in Japanese patients with relapsed or refractory chronic lymphocytic leukemia and small lymphocytic lymphoma. Jpn J Clin Oncol. 2013 May;43(5):466-75. doi: 10.1093/jjco/hyt022. Epub 2013 Feb 28.
• [5] FDA Approved Drug Products: ARZERRA (ofatumumab) injection, for intravenous use
• [6] Veve MP, Wagner JL: Lefamulin: Review of a Promising Novel Pleuromutilin Antibiotic. Pharmacotherapy. 2018 Sep;38(9):935-946. doi: 10.1002/phar.2166. Epub 2018 Aug 20.
• [7] Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
• [8] Product Information. Arava (leflunomide). Hoechst Marion-Roussel Inc, Kansas City, MO.
• [9] Product Information. Vumerity (diroximel fumarate). Alkermes, Inc, Cambridge, MA.
• [10] Cerner Multum, Inc. "Australian Product Information.".
• [11] Product Information. Gilenya (fingolimod). Novartis Pharmaceuticals, East Hanover, NJ.
• [12] Product Information. Ocrevus (ocrelizumab). Genentech, South San Francisco, CA.
• [13] Cerner Multum, Inc. "UK Summary of Product Characteristics.".
• [14] Product Information. Cimzia (certolizumab). UCB Pharma Inc, Smyrna, GA.
• [15] CDC. Centers for Disease Control and Prevention/ "Recommendations of the advisory committtee on immunization practices (ACIP): use of vaccines and immune globulins in persons with altered immunocompetence." MMWR Morb Mortal Wkly Rep 42(RR-04) (1993): 1-18. [PMID: 20300058]