Identification
NameDenosumab
Accession NumberDB06643
TypeBiotech
GroupsApproved
Description

Denosumab is a novel, fully human IgG2 monoclonal antibody specific to receptor activator of nuclear factor kappa-B ligand (RANKL), suppresses bone resorption markers in patients with a variety of metastatic tumors and is being investigated in multiple clinical trials for the prevention and treatment of bone metastases. Chemically, it consists of 2 heavy and 2 light chains. Each light chain consists of 215 amino acids. Each heavy chain consists of 448 amino acids with 4 intramolecular disulfides. FDA approved on June 1, 2010.

Protein structureDb06643
Related Articles
Protein chemical formulaC6404H9912N1724O2004S50
Protein average weight144700.0 Da
Sequences
> Denosumab αOPGL-1 heavy chain sequence
EVQLLESGGGLVQPGGSLRLSCAASGFTFSSYAMSWVRQAPGKGLEWVSGITGSGGSTYY
ADSVKGRFTISRDNSKNTLYLQMNSLRAEDTAVYYCAKDPGTTVIMSWFDPWGQGTLVTV
SSASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQ
SSGLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSCDKTHTCPPCPAPELL
GGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQ
YNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSR
DELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKS
RWQQGNVFSCSVMHEALHNHYTQKSLSLSPGK
> Denosumab αOPGL-1 light chain sequence
EIVLTQSPGTLSLSPGERATLSCRASQSVRGRYLAWYQQKPGQAPRLLIYGASSRATGIP
DRFSGSGSGTDFTLTISRLEPEDFAVFYCQQYGSSPRTFGQGTKVEIKRTVAAPSVFIFP
PSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTL
TLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
Download FASTA Format
SynonymsNot Available
External IDs AMG-162
Product Ingredients Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
ProliaSolution60 mgSubcutaneousAmgen2010-08-12Not applicableCanada
ProliaSolution60 mgSubcutaneousAmgenNot applicableNot applicableCanada
ProliaInjection60 mg/mLSubcutaneousAmgen2010-06-05Not applicableUs
XgevaInjection, solution120 mgSubcutaneousAmgen Europe B.V.2011-07-13Not applicableEu
XgevaSolution120 mgSubcutaneousAmgen2011-06-06Not applicableCanada
XgevaInjection, solution120 mgSubcutaneousAmgen Europe B.V.2011-07-13Not applicableEu
XgevaInjection120 mg/1.7mLSubcutaneousAmgen2010-11-18Not applicableUs
XgevaInjection, solution120 mgSubcutaneousAmgen Europe B.V.2011-07-13Not applicableEu
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
RanmarkDaiichi Sankyo
Brand mixturesNot Available
Categories
UNII4EQZ6YO2HI
CAS number615258-40-7
Pharmacology
Indication

Prolia is indicated for the treatment of postmenopausal women with osteoporosis at high risk for fracture. It reduces the incidence of vertebral, nonvertebral, and hip fractures. Prolia is also indicated as a treatment to increase bone mass in women at high risk for fracture receiving adjuvant aromatase inhibitor therapy for breast cancer. It can also be used in men with osteoporosis at high risk for fracture or in men receiving androgen deprivation therapy for nonmetastatic prostate cancer to increase bone mass. Xgeva is indicated for the prevention of skeletal-related events in patients with bone metastases from solid tumors.

Structured Indications
Pharmacodynamics

In clinical studies, treatment with 60 mg of Prolia resulted in reduction in the bone resorption marker serum type 1 C-telopeptide (CTX) by approximately 85% by 3 days. Consistent with the physiological coupling of bone formation and resorption in skeletal remodeling, subsequent reductions in bone formation markers (i.e. osteocalcin and procollagen type 1 N-terminal peptide [PlNP]) were observed starting 1 month after the first dose of Prolia.

Mechanism of action

Denosumab is designed to target RANKL (RANK ligand), a protein that acts as the primary signal to promote bone removal/resorption. In many bone loss conditions, RANKL overwhelms the body's natural defense against bone destruction. Denosumab prevents RANKL from activating its receptor, RANK, on the surface of osteoclasts and their precursors. Prevention of the RANKL/RANK interaction inhibits osteoclast formation, function, and survival, thereby decreasing bone resorption and increasing bone mass and strength in both cortical and trabecular bone.

TargetKindPharmacological actionActionsOrganismUniProt ID
Tumor necrosis factor ligand superfamily member 11Proteinyes
antibody
HumanO14788 details
Related Articles
Absorption

When 60 mg of denosumab was subcutaneously administered to healthy subjects after fasting for 12 hours, the pharmacokinetic parameters are as follows: Cmax = 6.75 mcg/mL; Tmax= 10 days (range of 3 to 21 days); AUC (0-16 weeks) = 316 mcg•day/mL. Denosumab does not accumulate following multiple doses once every 6 months. The pharmacokinetics of denosumab were not affected by the formation of antibodies.

Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half life

25.4 days

ClearanceNot Available
Toxicity

In patients with postmenopausal osteoporosis, the most common adverse reactions (> 5% and more common than placebo) were: back pain, pain in extremity, hypercholesterolemia, musculoskeletal pain, and cystitis. Pancreatitis has been reported in clinical trials. In male patients with osteoporosis, the most common adverse reactions (> 5% and more common than placebo) were: back pain, arthralgia, and nasopharyngitis. In patients experiencing bone loss due to hormone ablation for cancer, the most common adverse reactions (≥ 10% and more common than placebo) were: arthralgia and back pain. Pain in extremity and musculoskeletal pain have also been reported in clinical trials

Affected organisms
  • Humans and other mammals
PathwaysNot Available
Pharmacogenomic Effects/ADRs Not Available
Interactions
Drug Interactions
DrugInteractionDrug group
2-MethoxyethanolThe risk or severity of adverse effects can be increased when Denosumab is combined with 2-Methoxyethanol.Experimental
AbataceptThe risk or severity of adverse effects can be increased when Denosumab is combined with Abatacept.Approved
AdalimumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Adalimumab.Approved
Adefovir DipivoxilThe risk or severity of adverse effects can be increased when Denosumab is combined with Adefovir Dipivoxil.Approved, Investigational
AfelimomabThe risk or severity of adverse effects can be increased when Denosumab is combined with Afelimomab.Investigational
AlefaceptThe risk or severity of adverse effects can be increased when Denosumab is combined with Alefacept.Approved, Withdrawn
AlemtuzumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Alemtuzumab.Approved, Investigational
AltretamineThe risk or severity of adverse effects can be increased when Denosumab is combined with Altretamine.Approved
AmsacrineThe risk or severity of adverse effects can be increased when Denosumab is combined with Amsacrine.Approved
AnakinraThe risk or severity of adverse effects can be increased when Denosumab is combined with Anakinra.Approved
Antithymocyte immunoglobulin (rabbit)The risk or severity of adverse effects can be increased when Denosumab is combined with Anti-thymocyte Globulin (Rabbit).Approved
ApremilastThe risk or severity of adverse effects can be increased when Denosumab is combined with Apremilast.Approved, Investigational
AzacitidineThe risk or severity of adverse effects can be increased when Denosumab is combined with Azacitidine.Approved, Investigational
AzathioprineThe risk or severity of adverse effects can be increased when Denosumab is combined with Azathioprine.Approved
BasiliximabThe risk or severity of adverse effects can be increased when Denosumab is combined with Basiliximab.Approved, Investigational
BelataceptThe risk or severity of adverse effects can be increased when Denosumab is combined with Belatacept.Approved
BelimumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Belimumab.Approved
BetamethasoneThe risk or severity of adverse effects can be increased when Denosumab is combined with Betamethasone.Approved, Vet Approved
BleomycinThe risk or severity of adverse effects can be increased when Denosumab is combined with Bleomycin.Approved
BlinatumomabThe risk or severity of adverse effects can be increased when Denosumab is combined with Blinatumomab.Approved
Brentuximab vedotinThe risk or severity of adverse effects can be increased when Denosumab is combined with Brentuximab vedotin.Approved
BriakinumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Briakinumab.Investigational
BrodalumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Amg 827.Approved, Investigational
BudesonideThe risk or severity of adverse effects can be increased when Denosumab is combined with Budesonide.Approved
BusulfanThe risk or severity of adverse effects can be increased when Denosumab is combined with Busulfan.Approved, Investigational
CabazitaxelThe risk or severity of adverse effects can be increased when Denosumab is combined with Cabazitaxel.Approved
CanakinumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Canakinumab.Approved, Investigational
CapecitabineThe risk or severity of adverse effects can be increased when Denosumab is combined with Capecitabine.Approved, Investigational
CarboplatinThe risk or severity of adverse effects can be increased when Denosumab is combined with Carboplatin.Approved
CarmustineThe risk or severity of adverse effects can be increased when Denosumab is combined with Carmustine.Approved
CastanospermineThe risk or severity of adverse effects can be increased when Denosumab is combined with Castanospermine.Experimental
Certolizumab pegolThe risk or severity of adverse effects can be increased when Denosumab is combined with Certolizumab pegol.Approved
ChlorambucilThe risk or severity of adverse effects can be increased when Denosumab is combined with Chlorambucil.Approved
CisplatinThe risk or severity of adverse effects can be increased when Denosumab is combined with Cisplatin.Approved
CladribineThe risk or severity of adverse effects can be increased when Denosumab is combined with Cladribine.Approved, Investigational
ClofarabineThe risk or severity of adverse effects can be increased when Denosumab is combined with Clofarabine.Approved, Investigational
CorticotropinThe risk or severity of adverse effects can be increased when Denosumab is combined with Corticotropin.Approved, Vet Approved
Cortisone acetateThe risk or severity of adverse effects can be increased when Denosumab is combined with Cortisone acetate.Approved
CyclophosphamideThe risk or severity of adverse effects can be increased when Denosumab is combined with Cyclophosphamide.Approved, Investigational
CyclosporineThe risk or severity of adverse effects can be increased when Denosumab is combined with Cyclosporine.Approved, Investigational, Vet Approved
CytarabineThe risk or severity of adverse effects can be increased when Denosumab is combined with Cytarabine.Approved, Investigational
DacarbazineThe risk or severity of adverse effects can be increased when Denosumab is combined with Dacarbazine.Approved, Investigational
DaclizumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Daclizumab.Approved, Investigational
DactinomycinThe risk or severity of adverse effects can be increased when Denosumab is combined with Dactinomycin.Approved
DasatinibThe risk or severity of adverse effects can be increased when Denosumab is combined with Dasatinib.Approved, Investigational
DaunorubicinThe risk or severity of adverse effects can be increased when Denosumab is combined with Daunorubicin.Approved
DexamethasoneThe risk or severity of adverse effects can be increased when Denosumab is combined with Dexamethasone.Approved, Investigational, Vet Approved
Dimethyl fumarateThe risk or severity of adverse effects can be increased when Denosumab is combined with Dimethyl fumarate.Approved, Investigational
DinutuximabThe risk or severity of adverse effects can be increased when Denosumab is combined with Dinutuximab.Approved
DocetaxelThe risk or severity of adverse effects can be increased when Denosumab is combined with Docetaxel.Approved, Investigational
DoxorubicinThe risk or severity of adverse effects can be increased when Denosumab is combined with Doxorubicin.Approved, Investigational
EculizumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Eculizumab.Approved, Investigational
EfalizumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Efalizumab.Approved, Investigational
EpirubicinThe risk or severity of adverse effects can be increased when Denosumab is combined with Epirubicin.Approved
EstramustineThe risk or severity of adverse effects can be increased when Denosumab is combined with Estramustine.Approved
EtanerceptThe risk or severity of adverse effects can be increased when Denosumab is combined with Etanercept.Approved, Investigational
EtoposideThe risk or severity of adverse effects can be increased when Denosumab is combined with Etoposide.Approved
EverolimusThe risk or severity of adverse effects can be increased when Denosumab is combined with Everolimus.Approved
FingolimodThe risk or severity of adverse effects can be increased when Denosumab is combined with Fingolimod.Approved, Investigational
FloxuridineThe risk or severity of adverse effects can be increased when Denosumab is combined with Floxuridine.Approved
FludarabineThe risk or severity of adverse effects can be increased when Denosumab is combined with Fludarabine.Approved
FludrocortisoneThe risk or severity of adverse effects can be increased when Denosumab is combined with Fludrocortisone.Approved
FluorouracilThe risk or severity of adverse effects can be increased when Denosumab is combined with Fluorouracil.Approved
G17DTThe therapeutic efficacy of G17DT can be decreased when used in combination with Denosumab.Investigational
Gallium nitrateThe risk or severity of adverse effects can be increased when Denosumab is combined with Gallium nitrate.Approved, Investigational
GemcitabineThe risk or severity of adverse effects can be increased when Denosumab is combined with Gemcitabine.Approved
Gemtuzumab ozogamicinThe risk or severity of adverse effects can be increased when Denosumab is combined with Gemtuzumab ozogamicin.Approved, Investigational, Withdrawn
Glatiramer AcetateThe risk or severity of adverse effects can be increased when Denosumab is combined with Glatiramer Acetate.Approved, Investigational
GlimepirideThe risk or severity of adverse effects can be increased when Denosumab is combined with Glimepiride.Approved
GolimumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Golimumab.Approved
Human C1-esterase inhibitorThe risk or severity of adverse effects can be increased when Denosumab is combined with C1 Esterase Inhibitor (Human).Approved
HydrocortisoneThe risk or severity of adverse effects can be increased when Denosumab is combined with Hydrocortisone.Approved, Vet Approved
HydroxyureaThe risk or severity of adverse effects can be increased when Denosumab is combined with Hydroxyurea.Approved
Ibritumomab tiuxetanThe risk or severity of adverse effects can be increased when Denosumab is combined with Ibritumomab tiuxetan.Approved
IbrutinibThe risk or severity of adverse effects can be increased when Denosumab is combined with Ibrutinib.Approved
IcatibantThe risk or severity of adverse effects can be increased when Denosumab is combined with Icatibant.Approved
IdarubicinThe risk or severity of adverse effects can be increased when Denosumab is combined with Idarubicin.Approved
IdelalisibThe risk or severity of adverse effects can be increased when Denosumab is combined with Idelalisib.Approved
IfosfamideThe risk or severity of adverse effects can be increased when Denosumab is combined with Ifosfamide.Approved
ImatinibThe risk or severity of adverse effects can be increased when Denosumab is combined with Imatinib.Approved
ImiquimodThe risk or severity of adverse effects can be increased when Denosumab is combined with Imiquimod.Approved, Investigational
InfliximabThe risk or severity of adverse effects can be increased when Denosumab is combined with Infliximab.Approved
INGN 201The therapeutic efficacy of INGN 201 can be decreased when used in combination with Denosumab.Investigational
INGN 225The therapeutic efficacy of INGN 225 can be decreased when used in combination with Denosumab.Investigational
IrinotecanThe risk or severity of adverse effects can be increased when Denosumab is combined with Irinotecan.Approved, Investigational
L-PhenylalanineThe risk or severity of adverse effects can be increased when Denosumab is combined with L-Phenylalanine.Approved, Nutraceutical
LeflunomideThe risk or severity of adverse effects can be increased when Denosumab is combined with Leflunomide.Approved, Investigational
LenalidomideThe risk or severity of adverse effects can be increased when Denosumab is combined with Lenalidomide.Approved
LomustineThe risk or severity of adverse effects can be increased when Denosumab is combined with Lomustine.Approved
MechlorethamineThe risk or severity of adverse effects can be increased when Denosumab is combined with Mechlorethamine.Approved
MelphalanThe risk or severity of adverse effects can be increased when Denosumab is combined with Melphalan.Approved
MepolizumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Mepolizumab.Approved, Investigational
MercaptopurineThe risk or severity of adverse effects can be increased when Denosumab is combined with Mercaptopurine.Approved
MethotrexateThe risk or severity of adverse effects can be increased when Denosumab is combined with Methotrexate.Approved
MethylprednisoloneThe risk or severity of adverse effects can be increased when Denosumab is combined with Methylprednisolone.Approved, Vet Approved
MitomycinThe risk or severity of adverse effects can be increased when Denosumab is combined with Mitomycin.Approved
MitoxantroneThe risk or severity of adverse effects can be increased when Denosumab is combined with Mitoxantrone.Approved, Investigational
MuromonabThe risk or severity of adverse effects can be increased when Denosumab is combined with Muromonab.Approved, Investigational
Mycophenolate mofetilThe risk or severity of adverse effects can be increased when Denosumab is combined with Mycophenolate mofetil.Approved, Investigational
Mycophenolic acidThe risk or severity of adverse effects can be increased when Denosumab is combined with Mycophenolic acid.Approved
NafamostatThe risk or severity of adverse effects can be increased when Denosumab is combined with Nafamostat.Approved, Investigational
NatalizumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Natalizumab.Approved, Investigational
NelarabineThe risk or severity of adverse effects can be increased when Denosumab is combined with Nelarabine.Approved, Investigational
NilotinibThe risk or severity of adverse effects can be increased when Denosumab is combined with Nilotinib.Approved, Investigational
ObinutuzumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Obinutuzumab.Approved
OxaliplatinThe risk or severity of adverse effects can be increased when Denosumab is combined with Oxaliplatin.Approved, Investigational
PaclitaxelThe risk or severity of adverse effects can be increased when Denosumab is combined with Paclitaxel.Approved, Vet Approved
PalbociclibThe risk or severity of adverse effects can be increased when Denosumab is combined with Palbociclib.Approved
PanobinostatThe risk or severity of adverse effects can be increased when Denosumab is combined with Panobinostat.Approved, Investigational
PazopanibThe risk or severity of adverse effects can be increased when Denosumab is combined with Pazopanib.Approved
PegaspargaseThe risk or severity of adverse effects can be increased when Denosumab is combined with Pegaspargase.Approved, Investigational
PemetrexedThe risk or severity of adverse effects can be increased when Denosumab is combined with Pemetrexed.Approved, Investigational
PentostatinThe risk or severity of adverse effects can be increased when Denosumab is combined with Pentostatin.Approved, Investigational
PimecrolimusThe risk or severity of adverse effects can be increased when Denosumab is combined with Pimecrolimus.Approved, Investigational
PirarubicinThe risk or severity of adverse effects can be increased when Denosumab is combined with Pirarubicin.Investigational
PirfenidoneThe risk or severity of adverse effects can be increased when Denosumab is combined with Pirfenidone.Investigational
PomalidomideThe risk or severity of adverse effects can be increased when Denosumab is combined with Pomalidomide.Approved
PralatrexateThe risk or severity of adverse effects can be increased when Denosumab is combined with Pralatrexate.Approved
PrednisoloneThe risk or severity of adverse effects can be increased when Denosumab is combined with Prednisolone.Approved, Vet Approved
PrednisoneThe risk or severity of adverse effects can be increased when Denosumab is combined with Prednisone.Approved, Vet Approved
ProcarbazineThe risk or severity of adverse effects can be increased when Denosumab is combined with Procarbazine.Approved
RilonaceptThe risk or severity of adverse effects can be increased when Denosumab is combined with Rilonacept.Approved
RindopepimutThe therapeutic efficacy of CDX-110 can be decreased when used in combination with Denosumab.Investigational
RituximabThe risk or severity of adverse effects can be increased when Denosumab is combined with Rituximab.Approved
RuxolitinibThe risk or severity of adverse effects can be increased when Denosumab is combined with Ruxolitinib.Approved
SecukinumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Secukinumab.Approved
SeocalcitolThe risk or severity of adverse effects can be increased when Denosumab is combined with Seocalcitol.Experimental
SiltuximabThe risk or severity of adverse effects can be increased when Denosumab is combined with Siltuximab.Approved
SirolimusThe risk or severity of adverse effects can be increased when Denosumab is combined with Sirolimus.Approved, Investigational
SorafenibThe risk or severity of adverse effects can be increased when Denosumab is combined with Sorafenib.Approved, Investigational
SRP 299The therapeutic efficacy of SRP 299 can be decreased when used in combination with Denosumab.Investigational
SteproninThe risk or severity of adverse effects can be increased when Denosumab is combined with Stepronin.Approved
StreptozocinThe risk or severity of adverse effects can be increased when Denosumab is combined with Streptozocin.Approved
SunitinibThe risk or severity of adverse effects can be increased when Denosumab is combined with Sunitinib.Approved, Investigational
TacrolimusThe risk or severity of adverse effects can be increased when Denosumab is combined with Tacrolimus.Approved, Investigational
TemozolomideThe risk or severity of adverse effects can be increased when Denosumab is combined with Temozolomide.Approved, Investigational
TemsirolimusThe risk or severity of adverse effects can be increased when Denosumab is combined with Temsirolimus.Approved
TeniposideThe risk or severity of adverse effects can be increased when Denosumab is combined with Teniposide.Approved
TeriflunomideThe risk or severity of adverse effects can be increased when Denosumab is combined with Teriflunomide.Approved
ThalidomideThe risk or severity of adverse effects can be increased when Denosumab is combined with Thalidomide.Approved, Investigational, Withdrawn
ThiotepaThe risk or severity of adverse effects can be increased when Denosumab is combined with Thiotepa.Approved
TioguanineThe risk or severity of adverse effects can be increased when Denosumab is combined with Tioguanine.Approved
TocilizumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Tocilizumab.Approved
TofacitinibThe risk or severity of adverse effects can be increased when Denosumab is combined with Tofacitinib.Approved, Investigational
TopotecanThe risk or severity of adverse effects can be increased when Denosumab is combined with Topotecan.Approved, Investigational
TositumomabThe risk or severity of adverse effects can be increased when Denosumab is combined with Tositumomab.Approved
TrabectedinThe risk or severity of adverse effects can be increased when Denosumab is combined with Trabectedin.Approved, Investigational
Trastuzumab emtansineThe risk or severity of adverse effects can be increased when Denosumab is combined with Trastuzumab emtansine.Approved
TretinoinThe risk or severity of adverse effects can be increased when Denosumab is combined with Tretinoin.Approved, Investigational, Nutraceutical
TriamcinoloneThe risk or severity of adverse effects can be increased when Denosumab is combined with Triamcinolone.Approved, Vet Approved
UstekinumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Ustekinumab.Approved, Investigational
VedolizumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Vedolizumab.Approved
VilanterolThe risk or severity of adverse effects can be increased when Denosumab is combined with Vilanterol.Approved
VinblastineThe risk or severity of adverse effects can be increased when Denosumab is combined with Vinblastine.Approved
VincristineThe risk or severity of adverse effects can be increased when Denosumab is combined with Vincristine.Approved, Investigational
VindesineThe risk or severity of adverse effects can be increased when Denosumab is combined with Vindesine.Approved
VinorelbineThe risk or severity of adverse effects can be increased when Denosumab is combined with Vinorelbine.Approved, Investigational
VoclosporinThe risk or severity of adverse effects can be increased when Denosumab is combined with Lx211.Investigational
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General References
  1. Malan J, Ettinger K, Naumann E, Beirne OR: The relationship of denosumab pharmacology and osteonecrosis of the jaws. Oral Surg Oral Med Oral Pathol Oral Radiol. 2012 Dec;114(6):671-6. doi: 10.1016/j.oooo.2012.08.439. [PubMed:23159111 ]
  2. Link [Link]
  3. Link [Link]
External Links
ATC CodesM05BX04
AHFS Codes
  • 92:24
PDB EntriesNot Available
FDA labelDownload (226 KB)
MSDSDownload (97.5 KB)
Clinical Trials
Clinical Trials
PhaseStatusPurposeConditionsCount
0RecruitingTreatmentCancer, Breast1
1CompletedNot AvailableHealthy Volunteers1
1CompletedBasic ScienceHealthy Volunteer, Female, Breast1
1CompletedBasic ScienceHypersensitivity, Delayed / Immune Tolerance/Drug Effects / Immunosuppression / Ultraviolet Rays1
1CompletedTreatmentHealthy Volunteers1
1CompletedTreatmentImpaired Renal Function1
1CompletedTreatmentPostmenopausal Osteoporosis (PMO)1
1CompletedTreatmentBone destruction1
1Not Yet RecruitingPreventionDisorder Related to Bone Marrow Transplantation1
1RecruitingPreventionArthroplasty, Replacement, Hip1
1RecruitingTreatmentAdvanced Cancers1
1TerminatedTreatmentBone destruction / One to five years postmenopausal / Osteopenia / Rheumatoid Arthritis1
1, 2Not Yet RecruitingTreatmentArthritis, Juvenile Rheumatoid / Bone destruction / Dermatomyositis / Glucocorticoid-induced Osteoporosis / Polyarthritis / Systemic Lupus Erythematosus (SLE) / Vasculitis1
1, 2RecruitingTreatmentCrohn's Disease (CD)1
2Active Not RecruitingTreatmentBenign GCT / Cancers / GCT / Giant Cell Tumors of Bone1
2Active Not RecruitingTreatmentEarly Stage Breast Cancer1
2Active Not RecruitingTreatmentInfertilities / Sperm / Testis1
2Active Not RecruitingTreatmentNeoplasms, Breast1
2Active Not RecruitingTreatmentNon-Small-Cell Lung Carcinoma (NSCLC)1
2Active Not RecruitingTreatmentBone destruction / Thalassemia Major (TM)1
2Active Not RecruitingTreatmentBone destruction1
2CompletedPreventionAmbulation Difficulty / Osteoarthritis, Hip1
2CompletedSupportive CareBone Metastases in Subjects With Advanced Breast Cancer / Cancer, Breast / Metastases1
2CompletedTreatmentCancer, Breast / Endocrine Cancer / Head and Neck Carcinoma / Hypercalcemia of Malignancy / Lung Cancers / Lymphoma, Hodgkins / Malignant Lymphomas / Malignant Neoplasm of Colon / Metastatic Cancers / Multiple Myeloma (MM) / Non-Hodgkin's Lymphoma (NHL) / Non-Small-Cell Lung Carcinoma (NSCLC) / Parathyroid Neoplasms / Renal Cancers / Thyroid Cancers1
2CompletedTreatmentGCT / Giant Cell Tumors of Bone1
2CompletedTreatmentLow Bone Mineral Density1
2CompletedTreatmentLow Bone Mineral Density / Postmenopausal Osteoporosis (PMO)1
2CompletedTreatmentOsteogenesis Imperfecta1
2CompletedTreatmentPostmenopausal Osteoporosis (PMO)1
2CompletedTreatmentRelapsed or Plateau-Phase Multiple Myeloma1
2CompletedTreatmentRheumatoid Arthritis1
2RecruitingPreventionAdult Idiopathic Generalized Osteoporosis1
2RecruitingPreventionOsteolysis1
2RecruitingTreatmentBreast Carcinoma Metastatic in the Bone / Circulating Tumor Cell Count / Estrogen Receptor Positive / HER2/Neu Negative / Progesterone Receptor Positive / Stage IV Breast Cancer1
2RecruitingTreatmentCalcific Aortic Stenosis1
2RecruitingTreatmentCancer, Breast3
2RecruitingTreatmentChildhood Osteosarcoma / Metastatic Osteosarcoma / Recurrent Osteosarcoma1
2RecruitingTreatmentGout Acute1
2RecruitingTreatmentHER2 Positive Breast Cancers / Inflammatory carcinoma of the breast / Invasive Ductal Breast Carcinoma / Malignant Neoplasm of Female Breast / Mucinous Breast Cancer Stage II / Tubular Breast Cancer Stage II / Tubular Breast Cancer Stage III1
2RecruitingTreatmentHands Osteoarthritis1
2RecruitingTreatmentMale Infertility1
2RecruitingTreatmentMultiple Myeloma (MM)1
2RecruitingTreatmentRevision Surgery of Total Hip Arthroplasty1
2RecruitingTreatmentBone destruction / Spinal Cord Injuries (SCI)1
2RecruitingTreatmentBone destruction1
3Active Not RecruitingSupportive CareBone Metastases / Cancers / Malignancies, Hematologic / Multiple Myeloma (MM) / Multiple Myeloma Bone Lesions / Oncology1
3Active Not RecruitingSupportive CareCancer, Breast1
3Active Not RecruitingTreatmentBone Metastases in Men With Hormone-Refractory Prostate Cancer / Bone Metastases in Subjects With Advanced Breast Cancer1
3Active Not RecruitingTreatmentCancer, Breast1
3Active Not RecruitingTreatmentRheumatoid Arthritis1
3CompletedPreventionHormone Refractory Prostate Cancer1
3CompletedSupportive CareBone Metastases3
3CompletedSupportive CareBone destruction / Cancers / Cataracts / Low Bone Mineral Density / Malignant Neoplasm of Prostate / Osteopenia1
3CompletedSupportive CareBone destruction / Low Bone Mass / Low Bone Mineral Density / Postmenopausal Osteoporosis (PMO)1
3CompletedTreatmentCancers / Carcinoma NOS / Castrate-resistant Prostate Cancer (CRPC) / Malignant Neoplasm of Prostate / Tumors1
3CompletedTreatmentCastrate-resistant Prostate Cancer (CRPC)1
3CompletedTreatmentBone destruction / Chronic Kidney Disease (CKD)1
3CompletedTreatmentFractures, Bone1
3CompletedTreatmentBone destruction / Low Bone Mass / Low Bone Mineral Density / Males With Osteoporosis / Osteopenia1
3CompletedTreatmentBone destruction / Low Bone Mineral Density / Osteopenia1
3CompletedTreatmentBone destruction / Osteopenia2
3CompletedTreatmentPostmenopausal Osteoporosis (PMO)7
3CompletedTreatmentBone destruction4
3Not Yet RecruitingTreatmentEvaluate the Safety and Efficacy of Denosumab in Pediatric Subjects With / Glucocorticoid-induced Osteoporosis1
3Not Yet RecruitingTreatmentHyperparathyroidism, Primary / Parathyroid Adenomas / Parathyroid Hyperplasia1
3Not Yet RecruitingTreatmentBone destruction / Thalassemia Majors (Beta-Thalassemia Major)1
3RecruitingSupportive CareBone Metastases / Metastatic Breast Cancer (MBC) / Metastatic Hormone Refractory Prostate Cancer1
3RecruitingTreatmentCharcot Joint of Foot1
3RecruitingTreatmentLung Cancer Non-small Cell Stage IV1
3RecruitingTreatmentOsteogenesis Imperfecta1
4Active Not RecruitingTreatmentPostmenopausal Osteoporosis (PMO)1
4CompletedPreventionBone Resorption1
4CompletedTreatmentHyperparathyroidism, Primary1
4CompletedTreatmentMetabolic Bone Disease1
4CompletedTreatmentPost Menopausal Osteoporosis1
4CompletedTreatmentPostmenopausal Osteoporosis (PMO)1
4CompletedTreatmentRheumatoid Arthritis1
4CompletedTreatmentBone destruction2
4Not Yet RecruitingTreatmentFemale With Osteoporosis and Chronic Kidney Disease1
4Not Yet RecruitingTreatmentSecondary Osteoporosis / Spinal Cord Injuries (SCI)1
4Not Yet RecruitingTreatmentBone destruction1
4RecruitingTreatmentCancer, Breast / Malignant Neoplasm of Prostate / Metastasis1
4RecruitingTreatmentBone destruction / Osteoporotic Fractures / Postmenopausal Osteoporosis (PMO)1
4RecruitingTreatmentPostmenopausal Osteoporosis (PMO)1
4RecruitingTreatmentBone destruction1
4SuspendedTreatmentBone Marrow Oedema Syndrome / High Turnover Bone Disease / Quality of Life1
4Unknown StatusPreventionOsteoarthritis, Hip1
4WithdrawnNot AvailableMetastatic Bone Disease / Tumors, Solid1
Not AvailableActive Not RecruitingNot AvailablePost Menopausal Osteoperosis, Male Osteoperosis1
Not AvailableActive Not RecruitingNot AvailablePost Menopausal Osteoporosis1
Not AvailableCompletedNot AvailableBone destruction / Fractures, Bone1
Not AvailableCompletedNot AvailablePostmenopausal Osteoporosis (PMO)1
Not AvailableCompletedPreventionAging / Bone Loss1
Not AvailableCompletedTreatmentPostmenopausal Osteoporosis (PMO)1
Not AvailableRecruitingNot AvailableBone destruction1
Not AvailableRecruitingTreatmentMalignant Neoplasm of Prostate1
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
InjectionSubcutaneous60 mg/mL
SolutionSubcutaneous60 mg
InjectionSubcutaneous120 mg/1.7mL
Injection, solutionSubcutaneous120 mg
SolutionSubcutaneous120 mg
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2257247 No2012-09-112018-04-15Canada
CA2274987 No2012-01-242017-12-22Canada
CA2285746 No2010-09-282018-04-15Canada
CA2328140 No2012-03-132019-05-13Canada
CA2400929 No2011-05-312021-02-23Canada
Properties
StateSolid
Experimental PropertiesNot Available
Taxonomy
DescriptionNot Available
KingdomOrganic Compounds
Super ClassOrganic Acids
ClassCarboxylic Acids and Derivatives
Sub ClassAmino Acids, Peptides, and Analogues
Direct ParentPeptides
Alternative ParentsNot Available
SubstituentsNot Available
Molecular FrameworkNot Available
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antibody
General Function:
Tumor necrosis factor receptor superfamily binding
Specific Function:
Cytokine that binds to TNFRSF11B/OPG and to TNFRSF11A/RANK. Osteoclast differentiation and activation factor. Augments the ability of dendritic cells to stimulate naive T-cell proliferation. May be an important regulator of interactions between T-cells and dendritic cells and may play a role in the regulation of the T-cell-dependent immune response. May also play an important role in enhanced b...
Gene Name:
TNFSF11
Uniprot ID:
O14788
Molecular Weight:
35477.81 Da
References
  1. Lipton A, Jun S: RANKL inhibition in the treatment of bone metastases. Curr Opin Support Palliat Care. 2008 Sep;2(3):197-203. doi: 10.1097/SPC.0b013e32830baac2. [PubMed:18685421 ]
  2. Westenfeld R, Ketteler M, Brandenburg VM: Anti-RANKL therapy--implications for the bone-vascular-axis in CKD? Denosumab in post-menopausal women with low bone mineral density. Nephrol Dial Transplant. 2006 Aug;21(8):2075-7. Epub 2006 May 15. [PubMed:16702197 ]
Drug created on March 19, 2008 10:43 / Updated on June 22, 2017 16:17