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Necitumumab

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From Wikipedia, the free encyclopedia

Recombinant human monoclonal antibody

Pharmaceutical compound

Necitumumab
Monoclonal antibody
NecitumumabFab (blue) bound to EGFR (green).PDB:6B3S
Type	Whole antibody
Source	Human
Target	EGFR
Clinical data
Trade names	Portrazza
AHFS/Drugs.com	Multum Consumer Information
License data	US DailyMed: Necitumumab
Routes of administration	Intravenous infusion
ATC code	L01FE03 (WHO)
Legal status
Legal status	CA: ℞-only^[1] US: ℞-only^[2]
Pharmacokinetic data
Eliminationhalf-life	~14 days
Identifiers
CAS Number	906805-06-9^N
DrugBank	DB09559^Y
ChemSpider	none
UNII	2BT4C47RUI
KEGG	D10018^N
Chemical and physical data
Formula	C₆₄₃₆H₉₉₅₈N₁₇₀₂O₂₀₂₀S₄₂
Molar mass	144844.87 g·mol⁻¹
^NY (what is this?) (verify)

Necitumumab (INN) is a recombinant humanIgG1 monoclonal antibody used as anantineoplastic, which is manufactured by Eli Lilly. It binds to theepidermal growth factor receptor (EGFR).^[3] The USFDA approved necitumumab under the brand namePortrazza for use withgemcitabine andcisplatin in previously untreated metastaticsquamous non-small-cell lung carcinoma (NSCLC).^[4]^[5]^[2] It was counterproductive in non-squamous non-small-cell lung carcinoma.^[2]^[6]

References

[edit]

^"Cancer therapies".Health Canada. 8 May 2018. Retrieved13 April 2024.
^^a ^b ^c"Portrazza- necitumumab solution".DailyMed. 15 December 2023. Retrieved26 October 2024.
^International Nonproprietary Names for Pharmaceutical Substances (INN, prepublication copy),World Health Organization.
^Chustecka Z (2015-11-22)."Necitumumab (Portrazza) Approved for Lung Cancer in US". Medscape.com. Retrieved2019-09-28.
^"Necitumumab".Approved Drugs. U.S. Food and Drug Administration. Archived fromthe original on 2017-01-11. Retrieved2019-12-16.
^Hand L (3 March 2015)."Necitumumab Fails in NSCLC".MedScape. Archived fromthe original on 2015-11-29. Retrieved2015-11-25.

Targeted cancer therapy /antineoplastic agents (L01)

CI monoclonal antibodies ("-mab")

Receptor tyrosine kinase	ErbB:HER1/EGFR (Cetuximab Panitumumab) HER2/neu (Pertuzumab Trastuzumab (+hyaluronidase) Trastuzumab emtansine Trastuzumab deruxtecan Zanidatamab )
Others for solid tumors	EpCAM (Catumaxomab Edrecolomab) VEGF-A (Bevacizumab)
Leukemia/lymphoma	lymphoid:CD3 (Glofitamab,Elranatamab,Mosunetuzumab),CD20 (Glofitamab Ibritumomab Mosunetuzumab Obinutuzumab Ofatumumab Rituximab Tositumomab),CD30 (Brentuximab),CD52 (Alemtuzumab) myeloid:CD33 (Gemtuzumab ozogamicin)
Other	Amivantamab (+hyaluronidase) Atezolizumab (+hyaluronidase) Avelumab Axatilimab Belantamab mafodotin Bermekimab Blinatumomab Cemiplimab Cosibelimab Daratumumab Dinutuximab beta Dostarlimab Durvalumab Elotuzumab Enfortumab vedotin Epcoritamab Inotuzumab ozogamicin Ipilimumab Isatuximab Linvoseltamab Loncastuximab tesirine Mirvetuximab soravtansine Mogamulizumab Moxetumomab pasudotox Naxitamab Necitumumab Nivolumab (+hyaluronidase,+relatlimab) Olaratumab Oportuzumab monatox Pembrolizumab (+berahyaluronidase alfa) Penpulimab Polatuzumab vedotin Prolgolimab Ramucirumab Retifanlimab Sabatolimab Sacituzumab govitecan Serplulimab Sugemalimab Tafasitamab Talquetamab Tarlatamab Teclistamab Tislelizumab Tisotumab vedotin Toripalimab Tremelimumab Zenocutuzumab Zolbetuximab

Tyrosine kinase inhibitors ("-nib")

Receptor tyrosine kinase

HER1/EGFR andHER2/neu

BRAF

RTK class III:C-kit andPDGFR (Avapritinib
Axitinib
Masitinib
Pazopanib
Ripretinib
Sorafenib
Sunitinib
Toceranib)
FLT3 (Lestaurtinib,Gilteritinib (AXL, ALK, LTK))

VEGFR

ALK

RET inhibitors:Entrectinib (ALK, ROS1, NTRK),Futibatinib (FGFR2),Infigratinib,Larotrectinib (NTRK),Pemigatinib (FGFR),Pralsetinib,Repotrectinib (ROS1, TRK, ALK),Selpercatinib (VEGFR, FGFR),Taletrectinib (ROS1),Vandetanib (VEGFR, EGFR).

c-MET inhibitors:Cabozantinib (VEGFR),Capmatinib,Crizotinib (ALK)

Non-receptor

bcr-abl

Src (Bosutinib
Dasatinib)

Janus kinase (JAK)

MAP2K (MEK)

EML4-ALK

Bruton's (BTK)

Other

fusion protein againstVEGF (Aflibercept)

proapoptotic peptide againstANXA2 andprohibitin (Adipotide)

exotoxin againstIL-2 (Denileukin diftitox)

mTOR inhibitors

hedgehog inhibitors

CDK inhibitors

KRAS inhibitors
- Adagrasib
- Sotorasib

Pi3K inhibitors

Menin inhibitors
- Revumenib
- Ziftomenib

Fibroblast growth factor receptor (FGFR) inhibitors
Erdafitinib
Futibatinib
Infigratinib
Pemigatinib

Monoclonal antibodies for tumors

Tumor

Human	Adecatumumab^§ Amivantamab (+hyaluronidase) Ascrinvacumab^§ Balstilimab^† Botensilimab Cixutumumab^§ Conatumumab^§ Cosibelimab Daratumumab Drozitumab^§ Duligotumab^§ Dusigitumab^§ Enfortumab vedotin Enoticumab^§ Figitumumab^§ Flanvotumab^§ Ganitumab^† Glembatumumab vedotin^† Intetumumab^§ Ipilimumab Iratumumab^§ Istiratumab Icrucumab^§ Lexatumumab^§ Linvoseltamab Lucatumumab^§ Mapatumumab^§ Narnatumab^§ Necitumumab Nesvacumab^§ Nivolumab^# (+hyaluronidase,+relatlimab) Ofatumumab Olaratumab^† Panitumumab Patritumab^§ Pritumumab^§ Radretumab^§ Ramucirumab Rilotumumab^† Robatumumab^§ Seribantumab^§ Sugemalimab Tarextumab^§ Tisotumab vedotin Teprotumumab^† Tovetumab^§ Vantictumab^§ Votumumab^§ Zalutumumab^†
Mouse	Abagovomab Altumomab pentetate Anatumomab mafenatox Arcitumomab Bectumomab Blinatumomab Capromab pendetide Detumomab Edrecolomab Ibritumomab tiuxetan Igovomab Lilotomab Minretumomab Mitumomab Nacolomab tafenatox Moxetumomab pasudotox Naptumomab estafenatox Oregovomab Pemtumomab^† Racotumomab Satumomab pendetide Solitomab Taplitumomab paptox Nofetumomab merpentan Pintumomab Tenatumomab Tositumomab
Chimeric	Amatuximab^§ Bavituximab^§ Brentuximab vedotin Carotuximab^† Cetuximab Derlotuximab biotin^§ Dinutuximab Ecromeximab^§ Ensituximab^§ Futuximab^§ Girentuximab^† Indatuximab ravtansine^§ Isatuximab Loncastuximab tesirine Margetuximab Mirvetuximab soravtansine Rituximab^# Siltuximab Ublituximab Zolbetuximab
Humanized	Abituzumab^§ Alemtuzumab Atezolizumab (+hyaluronidase) Axatilimab Belantamab mafodotin Bevacizumab Bivatuzumab mertansine^§ Brontictuzumab^§ Cantuzumab mertansine^§ Cantuzumab ravtansine^§ Cirmtuzumab Citatuzumab bogatox^§ Clivatuzumab tetraxetan Cofetuzumab pelidotin Dacetuzumab^§ Demcizumab^§ Dalotuzumab^§ Datopotamab deruxtecan Denintuzumab mafodotin^§ Elotuzumab Emactuzumab Emibetuzumab^§ Enoblituzumab^§ Epcoritamab Etaracizumab^§ Farletuzumab^§ Ficlatuzumab^§ Flotetuzumab^§ Gemtuzumab ozogamicin Glofitamab Imgatuzumab^§ Inotuzumab ozogamicin Labetuzumab^§ Lifastuzumab vedotin^§ Lintuzumab^§ Lorvotuzumab mertansine^§ Lumretuzumab^§ Matuzumab^§ Milatuzumab^§ Naxitamab Nimotuzumab^† Obinutuzumab Ocaratuzumab^§ Odronextamab Otlertuzumab^§ Onartuzumab^§ Oportuzumab monatox^† Parsatuzumab^§ Pembrolizumab^# (+berahyaluronidase alfa) Penpulimab Pertuzumab Pinatuzumab vedotin^§ Polatuzumab vedotin Rosmantuzumab Rovalpituzumab tesirine^† Sacituzumab govitecan Sibrotuzumab^§ Simtuzumab^§ Sofituzumab vedotin^§ Tacatuzumab tetraxetan^§ Tigatuzumab^§ Trastuzumab^# (+deruxtecan /+emtansine) Tucotuzumab celmoleukin^§ Vandortuzumab vedotin^§ Vanucizumab^§ Veltuzumab^§ Vorsetuzumab mafodotin^§ Zenocutuzumab
Rat/mouse hybrid	Catumaxomab Ertumaxomab^§
Chimeric + humanized	Depatuxizumab mafodotin^† Duvortuxizumab Ontuxizumab^§

^#WHO-EM
^‡Withdrawn from market
Clinical trials:
- ^†Phase III
- ^§Never to phase III

Growth factor receptor modulators

Angiopoietin

Agonists:Angiopoietin 1
Angiopoietin 4

Antagonists:Angiopoietin 2
Angiopoietin 3

Kinase inhibitors:Altiratinib
CE-245677
Rebastinib

Antibodies:Evinacumab (against angiopoietin 3)
Nesvacumab (against angiopoietin 2)

CNTF

EGF (ErbB)

EGF (ErbB1/HER1)	Agonists:Amphiregulin Betacellulin EGF (urogastrone) Epigen Epiregulin Heparin-binding EGF-like growth factor (HB-EGF) Murodermin Nepidermin Transforming growth factor alpha (TGFα) Kinase inhibitors:Afatinib Agerafenib Brigatinib Canertinib Dacomitinib Erlotinib Gefitinib Grandinin Icotinib Lapatinib Neratinib Osimertinib Vandetanib WHI-P 154 Antibodies:Cetuximab Depatuxizumab Depatuxizumab mafodotin Futuximab Imgatuzumab Matuzumab Necitumumab Nimotuzumab Panitumumab Zalutumumab
ErbB2/HER2	Agonists:Unknown/none Antibodies:Ertumaxomab Pertuzumab Trastuzumab Trastuzumab deruxtecan Trastuzumab duocarmazine Trastuzumab emtansine Kinase inhibitors:Afatinib Lapatinib Mubritinib Neratinib Tucatinib
ErbB3/HER3	Agonists:Neuregulins (heregulins) (1,2,6 (neuroglycan C)) Antibodies:Duligotumab Patritumab Seribantumab
ErbB4/HER4	Agonists:Betacellulin Epigen Heparin-binding EGF-like growth factor (HB-EGF) Neuregulins (heregulins) (1,2,3,4,5 (tomoregulin, TMEFF))

FGF

FGFR1	Agonists:Ersofermin FGF (1,2 (bFGF),3,4,5,6,8,10 (KGF2),20) Repifermin Selpercatinib Trafermin Velafermin
FGFR2	Agonists:Ersofermin FGF (1,2 (bFGF),3,4,5,6,7 (KGF),8,9,10 (KGF2),17,18,22) Palifermin Repifermin Selpercatinib Sprifermin Trafermin Antibodies:Aprutumab Aprutumab ixadotin Kinase inhibitors:Infigratinib
FGFR3	Agonists:Ersofermin FGF (1,2 (bFGF),4,8,9,18,23) Selpercatinib Sprifermin Trafermin Antibodies:Burosumab (against FGF23)
FGFR4	Agonists:Ersofermin FGF (1,2 (bFGF),4,6,8,9,19) Trafermin
Unsorted	Agonists:FGF15/19

HGF (c-Met)

Agonists:Fosgonimeton
Hepatocyte growth factor

Potentiators:Dihexa (PNB-0408)

IGF

IGF-1	Agonists:des(1-3)IGF-1 Insulin-like growth factor-1 (somatomedin C) IGF-1 LR3 Insulin-like growth factor-2 (somatomedin A) Insulin Mecasermin Mecasermin rinfabate Kinase inhibitors:BMS-754807 Linsitinib NVP-ADW742 NVP-AEW541 OSl-906 Antibodies:AVE-1642 Cixutumumab Dalotuzumab Figitumumab Ganitumab Robatumumab R1507 Teprotumumab Xentuzumab (against IGF-1 and IGF-2)
IGF-2	Agonists:Insulin-like growth factor-2 (somatomedin A) Antibodies:Dusigitumab Xentuzumab (against IGF-1 and IGF-2)
Others	Binding proteins:IGFBP (1,2,3,4,5,6,7) Cleavage products/derivatives with unknown target:Glypromate (GPE, (1-3)IGF-1) Trofinetide

LNGF (p75^NTR)

Antibodies:Against NGF:ABT-110 (PG110)
ASP-6294
Fasinumab
Frunevetmab
Fulranumab
MEDI-578
Ranevetmab
Tanezumab

Aptamers:Against NGF:RBM-004

Decoy receptors:LEVI-04 (p75^NTR-Fc)

PDGF

Agonists:Becaplermin
Platelet-derived growth factor (A,B,C,D)

RET (GFL)

GFRα1	Agonists:Glial cell line-derived neurotrophic factor (GDNF) Liatermin Kinase inhibitors:Vandetanib
GFRα2	Agonists:Neurturin (NRTN) Kinase inhibitors:Vandetanib
GFRα3	Agonists:Artemin (ARTN) Kinase inhibitors:Vandetanib
GFRα4	Agonists:Persephin (PSPN) Kinase inhibitors:Vandetanib
Unsorted	Kinase inhibitors:Agerafenib

SCF (c-Kit)

Agonists:Ancestim
Stem cell factor

TGFβ

Seehere instead.

Trk

TrkA	Agonists:Amitriptyline BNN-20 BNN-27 Cenegermin DHEA DHEA-S Gambogic amide NGF Tavilermide Antagonists:ALE-0540 Dexamethasone FX007 Testosterone Positive allosteric modulators:ACD856 ACD857 Ponazuril (ACD855) Toltrazuril Negative allosteric modulators:VM-902A Kinase inhibitors:Altiratinib AZD-6918 CE-245677 CH-7057288 DS-6051 Entrectinib GZ-389988 K252a Larotrectinib Lestaurtinib Milciclib ONO-4474 ONO-5390556 PLX-7486 Rebastinib SNA-120 (pegylated K252a)) Antibodies:Against TrkA:GBR-900;Against NGF:ABT-110 (PG110) ASP-6294 Fasinumab Frunevetmab Fulranumab MEDI-578 Ranevetmab Tanezumab Aptamers:Against NGF:RBM-004 Decoy receptors:ReN-1820 (TrkAd5)
TrkB	Agonists:3,7-DHF 3,7,8,2'-THF 4'-DMA-7,8-DHF 7,3'-DHF 7,8-DHF 7,8,2'-THF 7,8,3'-THF Amitriptyline Braegen-02 BDNF BNN-20 Deoxygedunin Diosmetin DMAQ-B1 HIOC LM22A-4 N-Acetylserotonin NT-3 NT-4 Norwogonin (5,7,8-THF) R7 R13 (BrAD-R13, Braegen-01) TDP6 Antagonists:ANA-12 Cyclotraxin B Gossypetin (3,5,7,8,3',4'-HHF) Ligands:DHEA Positive allosteric modulators:ACD856 ACD857 Ponazuril (ACD855) Toltrazuril Kinase inhibitors:Altiratinib AZD-6918 CE-245677 CH-7057288 DS-6051 Entrectinib GZ-389988 K252a Larotrectinib Lestaurtinib ONO-4474 ONO-5390556 PLX-7486
TrkC	Agonists:BNN-20 DHEA NT-3 Positive allosteric modulators:ACD856 Kinase inhibitors:Altiratinib AZD-6918 CE-245677 CH-7057288 DS-6051 Entrectinib GZ-389988 K252a Larotrectinib Lestaurtinib ONO-4474 ONO-5390556 PLX-7486