Romosozumab
Romosozumab Uses, Dosage, Side Effects, Food Interaction and all others data.
Romosozumab is a humanized monoclonal antibody indicated for the treatment of osteoperosis in postmenopausal women at high risk of fracture and patients who have failed in other treatments or are intolerant to other osteoperosis therapies. Romosozumab prevents bone resorption and induces the formation of bone though it is associated with an increased risk of cardiac death, heart attack, and stroke in one study. In a comparison study of post menopausal women with osteoporosis and a past fracture, romosozumab for 12 months followed by alendronic acid for 12 months was superior to alendronic acid alone for 24 months. Romosozumab also demonstrates a faster and larger increase in bone density than teriparatide. Romosozumab is marketed in the United States by Amgen under the brand name Evinity. Romosozumab was granted FDA approval on April 9,2019.
Romosozumab is a subcutaneously injected humanized monoclonal antibody that inhibits the secreted protein sclerostin. Inhibition of this protein allows Wnt signalling in osteoblasts to promote bone formation and allows for the inhibition of receptor activator of nuclear factor kappa-beta-ligand (RANKL) mediated bone resorption by osteoclasts.
| Trade Name | Romosozumab |
| Availability | Prescription only |
| Generic | Romosozumab |
| Romosozumab Other Names | Romosozumab, romosozumab-aqqg |
| Related Drugs | Prolia, hydrochlorothiazide, alendronate, calcitonin, Fosamax, Tymlos |
| Weight | 105mg/1.17ml |
| Type | Subcutaneous solution |
| Weight | 145805.0 Da |
| Protein binding | Monoclonal antibodies are generally not protein bound. In about 10% to 18.1% of cases patients develop antibodies against romosozumab. 4.7% of the patients developed neutralizing antibodies. The presence of antibodies against romosozumab can reduce the availability of romosozumab by 22%, and 63% in the case of neutralizing antibodies. |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Romosozumab is a monoclonal antibody used to treat osteoporosis in postmenopausal women at high risk of fracture, patients who are intolerant of other treatments, or patients who have failed other treatments.
Romosozumab is indicated for the treatment of osteoporosis in post menopausal women at high risk of fractures and also in patients with osteoperosis who are intolerant to other treatments or who have failed in other treatments.
Romosozumab is also used to associated treatment for these conditions: Osteoporosis
How Romosozumab works
Osteocytes secrete sclerostin which inhibits bone formation by binding to low-density lipoprotein (LDL) receptor-related proteins 5 and 6 of osteoblasts, inhibiting the Wnt signal pathway.
Romosozumab targets and inhibits the protein sclerostin, thereby preventing inhibition of bone formation by allowing Wnt to bind to LDL receptor-related proteins 5 and 6. Activation of the Wnt pathways leads to downstream signalling, translocation of beta catenin to the osteoblast nucleus where it promotes survival and proliferation of osteoblasts.
Sclerostin also promotes bone resorption through increasing production of receptor activator of nuclear factor kappa-beta-ligand (RANKL).
Romosozumab's inhibition of sclerostin also inhibits the increase in RANKL dependant increases in osteoclast activity and bone resorption. Both effects from the same therapy have not been seen in other osteoporosis treatments to date.
Toxicity
There are no significant differences in pharmacokinetics cross age, sex, race, progression of osteoporosis, past history of alendronic acid prescribing, and all stages of renal impairment. However, patients with severe renal impairment or who are on dialysis are at an increased risk of hypocalcemia. A patient's weight will affect their level of romosozumab exposure.
Romosozumab has not been shown to be associated with carcinogenicity or impairment of fertility, and is not expected to be mutagenic.
Romosozumab is not indicated in pregnancy, lactation, or pedatric patients. Romosozumab is associated with skeletal defects in the offspring of rats given romosozumab and is detected in the excreted milk.
Romosozumab is currently undergoing post marketing surveillance to ensure the risk of major adverse cardiac events is not being underestimated. There is currently an expected hazard ratio of 1.30 compared to current treatments for osteoporosis, though hip and vertebral fractures may have an equal impact on overall quality of life.
Food Interaction
- Administer calcium supplement. Ensure adequate calcium supplementation.
- Administer vitamin supplements. Ensure adequate vitamin D supplementation.
Romosozumab Drug Interaction
Moderate: denosumabUnknown: lactobacillus acidophilus, aspirin, diphenhydramine, losartan, rosuvastatin, duloxetine, diltiazem, clonazepam, linaclotide, morphine, morphine, pravastatin, omeprazole, montelukast, levothyroxine, fluticasone / umeclidinium / vilanterol, plecanatide, ascorbic acid, cholecalciferol
Romosozumab Disease Interaction
Major: hypocalcemia, myocardial infarction/strokeModerate: osteonecrosis of the jaw
Volume of Distribution
3.92L.
Elimination Route
Romosozumab reaches peak concentration within 2 to 7 days with a median time of 5 days. Subcutaneous bioavailability is 50 to 70%.
Half Life
12.8 days.
Clearance
0.38mL/hr/kg.
Elimination Route
Monoclonal antibodies are eventually phagocytosed and broken down to smaller peptides and amino acids which are eliminated in a similar fashion to other proteins.
Innovators Monograph
You find simplified version here Romosozumab
