Buy Prolia® syringe 60 mg
  • Buy Prolia® syringe 60 mg

Prolia® [Denosumab]

Amgen Manewackering Limited
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Clinical Pharmacology

Denosumab is a fully human monoclonal antibody (IgG2), which has a high affinity and specificity for the ligand receptor for the nuclear factor Kappa B activator (RANKL) and thus prevents the activation of the single receptor RANKL - nuclear factor activator kV (RANK) located on the surface of osteoclasts and their predecessors. Thus, preventing the interaction of RANKL / RANK inhibits the formation, activation and longevity of osteoclasts. As a result, denosumab reduces bone resorption and increases the mass and strength of the cortical and trabecular bone layers.
Pharmacodynamic effects:
The administration of denosumab at a dose of 60 mg resulted in a rapid decrease in serum concentrations of the bone tissue resorption marker 1C-telopeptide (CTX) —about 70% within 6 hours after s / c administration and approximately 85% over the next 3 days. The decrease in CTX concentration remained stable in the 6-month interval between dosing. The rate of decrease in serum CTX concentration partially decreased with a decrease in serum denosumab concentration, which reflects the reversibility of the effect of denosumab on bone remodeling. These effects were observed throughout the course of treatment. According to the physiological relationship of the processes of formation and resorption during bone tissue remodeling, a decrease in the content of bone formation markers (for example, bone-specific alkaline phosphatase and serum N-terminal propeptide type 1 collagen) was observed from the first month after the first dose of denosumab. Bone remodeling markers (markers of bone formation and bone resorption), as a rule, reached concentrations of the period before the start of treatment no later than 9 months after taking the last dose of the drug. After the resumption of treatment with denosumab, the degree of decrease in CTX concentrations was similar to the degree of decrease in the concentration of CTX at the beginning of the course of treatment with denosumab.
It was shown that a switch from treatment with alendronic acid (average duration of use - 3 years) to denosumab leads to an additional decrease in serum CTX concentration compared with a group of postmenopausal women with low bone mass, who continued treatment with alendronic acid. At the same time, changes in serum calcium were similar in both groups.
In experimental studies, inhibition of RANK / RANKL simultaneously with the binding of osteoprotegerin to the Fc fragment (OPG-Fc), resulted in slower bone growth and impaired teething. Therefore, treatment with denosumab can inhibit the growth of bones with open growth zones in children and lead to impaired teething.
Immunogenicity:
Denosumab is a human monoclonal antibody, therefore, as for other protein drugs of a nature, there is a theoretical risk of immunogenicity. More than 13,000 patients were examined for the formation of binding antibodies using the sensitive electrochemiluminescence method in combination with immunological analysis. In less than 1% of patients who had taken denosumab for 5 years, antibodies were detected (including preexisting, transient and growing). Seropositive patients were further examined for the formation of neutralizing antibodies using chemiluminescent analysis in an in vitro cell culture; no neutralizing antibodies were detected. There were no changes in pharmacokinetic profile, toxic profile or clinical response due to the formation of antibodies.
Clinical efficacy
Postmenopausal osteoporosis treatment
In women with postmenopausal osteoporosis, Prolia increases bone mineral density (BMD), reduces the incidence of hip fractures, vertebral and non-vertebral fractures.The efficacy and safety of denosumab in the treatment of postmenopausal osteoporosis was proven in a study lasting 3 years. The results of the study show that denosumab significantly, compared with placebo, reduces the risk of vertebral and non-vertebral fractures, hip fractures in women with postmenopausal osteoporosis. The study included 7808 women, of whom 23% had frequent vertebral fractures. All three efficacy endpoints for fractures reached statistically significant values, assessed by a predetermined sequential testing pattern.
Reducing the risk of new vertebral fractures when using denosumab for more than 3 years remained stable and significant. The risk was reduced regardless of the 10-year probability of major osteoporotic fractures. The history of vertebral fractures, nonvertebral fractures, age, patients, BMD, bone remodeling and previous therapy for osteoporosis did not affect the risk reduction either.
In women older than 75, post-menopausal denosumab reduced the incidence of new vertebral fractures and, according to post hoc analysis, reduced the incidence of hip fractures.
A decrease in the incidence of non-vertebral fractures was observed regardless of the 10-year probability of the occurrence of major osteoporotic fractures.
Denosumab significantly, compared with placebo, increased BMD in all anatomical areas. BMD was determined 1 year, 2 and 3 years after the start of therapy. A similar effect on BMD is observed in the lumbar spine, regardless of age, race, body mass index (BMI), BMD, and bone remodeling.
Histological studies confirmed the normal architectonics of the bone and, as expected, a decrease in bone remodeling compared with placebo. No pathological changes, including fibrosis, osteomalacia and impaired bone marrow architecture, were noted.
Clinical efficacy in the treatment of bone loss caused by hormone therapy or aromatase inhibitor therapy:
Treatment of bone loss caused by androgen deprivation:
The efficacy and safety of denosumab in treating bone loss associated with decreased androgen concentration was proven in a 3-year study that included 1,468 patients with non-metastatic prostate cancer.
A significant increase in BMD was determined in the lumbar spine, the entire femur, the femoral neck, and the skew of the femur 1 month after taking the first dose. The increase in BMD in the lumbar spine did not depend on age, race, geographic region, BMI, initial values
BMD, bone remodeling; the duration of hormone-deprivation therapy and the presence of a vertebral fracture in history.
Denosumab significantly reduced the risk of new vertebral fractures over the course of 3 years of use. Risk reduction was observed after 1 year and 2 years after the start of therapy. Denosumab also reduced the risk of more than one osteoporotic fracture of any location.
Treatment of bone loss in women receiving aromatase inhibitor therapy for breast jelly
The efficacy and safety of denosumab in the treatment of bone loss caused by adjuvant therapy with an aromatase inhibitor was evaluated in a 2-year study that included 252 patients with non-metastatic breast cancer. Denosumab significantly increased the IPC in all anatomical areas, compared with placebo, for 2 years. An increase in BMD was observed in the lumbar spine a month after taking the first dose.A positive effect on BMD in the lumbar spine was noted regardless of age, duration of therapy with an aromatase inhibitor, BMI, prior chemotherapy, prior use of the selective estrogen receptor modulator (MRE) and time elapsed from the onset of menopause.

Indications

- treatment of postmenopausal osteoporosis;
- treatment of bone loss in women receiving therapy with aromatase inhibitors for breast cancer and in men with prostate cancer receiving hormone-deprivation therapy.

Composition

1 syringe:
- Denozumab 60 mg
Excipients: sorbitol (E420) 47 mg, glacial acetic acid 1 mg, sodium hydroxide to pH 5.0-5.5, polysorbate 20 0.1 mg, water d / and up to 1 ml.

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Prolia® [Denosumab]

Dosage and Administration

Introduction:
Conducting an injection requires prior training - see the recommendations for the introduction of the drug, given at the end of this instruction.
The recommended dose of Prolia is one sc injection of 60 mg every 6 months. During the course of treatment it is recommended to take calcium supplements and vitamin D.
Children:
Prolia is not recommended for use in pediatrics, as the efficacy and safety of this drug has not been studied in this age group.
Elderly patients:
Based on the available data on the efficacy and safety of the drug in this age group, no adjustment of the dosage regimen of the drug is required.
Renal failure:
Based on the available data on the efficacy and safety of the drug in this group of patients, no adjustment of the dosage regimen of the drug is required.
In patients with severe renal failure (creatinine clearance) Hepatic failure:
Efficiency and safety have not been studied.

Instructions for use:
You should evaluate the solution before administration for the presence of inclusions or discoloration. The solution can not be used in turbidity or color change. Do not shake.
To avoid discomfort at the injection site, warm Prolium solution to room temperature (up to 25 ° C) before injection, and then slowly inject the entire contents of the pre-filled syringe. Dispose of the syringe with the remnants of the drug.
Any amount of unused drug or unused materials must be disposed of in accordance with local requirements.

Adverse reactions

Data obtained from controlled use in clinical studies.
Undesirable reactions are given by organ system classes in terms of the Medical Dictionary of Regulatory Activities (MedDRA).
The incidence of adverse events was classified as follows: very often (≥1 / 10), often (≥1 / 100,

In each group of organ systems and message frequencies, adverse reactions are listed in descending order of severity.

Organ system class Frequency Unwanted reaction
Infections and invasions Infrequently subcutaneous inflammation
On the part of metabolism and electrolyte metabolism Very rarely hypocalcemia
On the part of the organ of vision Often cataracts in men receiving androgen deprivation therapy for prostate cancer
From the skin and subcutaneous fat Infrequently eczema, including dermatitis, allergic dermatitis, atopic dermatitis, contact dermatitis
From the musculoskeletal system and connective tissue Often
Seldom
Pain in limbs
Osteonecrosis of the jaw

- hypocalcemia;
- Hypersensitivity to any of the components of the drug Prolia.

Drug interactions

Research on drug interactions has not been conducted.
The drug should not be mixed with other drugs.

Pregnancy and Lactation

There is no data on the use of the drug during pregnancy. Prolia is not recommended for use in pregnant women.
In toxicological studies on lower primates, it was shown that at doses 100-fold higher than those recommended for clinical use, denosumab did not affect fertility or fetal development.
Experiments on mice with the genes turned off showed that the absence of RANKL can lead to disruption of the development of lymph nodes in the fetus, and in the postnatal period can cause a violation of teething and bone growth; may also affect the maturation of the mammary gland, which may lead to a weakening of lactation.
It is not known whether denosumab is excreted into breast milk. Since it is known that potentially denosumab can cause undesirable reactions in infants, it is necessary either to stop breastfeeding, or to stop the drug Prolia.

Special instructions

It is recommended that calcium and vitamin D supplements be taken while using Prolia.
Hypocalcemia can be adjusted by taking calcium and vitamin D supplements in adequate doses before starting denosumab therapy. It is recommended to control the concentration of calcium in patients prone to hypocalcemia.
Patients receiving Prolia may develop infections of the skin and its appendages (mainly inflammation of the subcutaneous tissue), in some cases requiring hospitalization. Such reactions were more frequently reported for the denosumab group (0.4%) than the placebo group (0.1%). However, the overall incidence of skin infections is comparable in the denosumab and placebo groups. Patients should be instructed to promptly seek medical attention if symptoms and signs of inflammation of the subcutaneous tissue develop.
In patients with advanced cancer who received 120 mg of denosumab every 4 weeks, osteonecrosis of the jaw was reported. There are some reports of osteonecrosis of the jaw at a dose of 60 mg every 6 months.
Persons allergic to latex should not touch the rubber needle cap (a derivative of latex).
Influence on ability to drive motor transport and control mechanisms:
Studies on the effect of Proline on the ability to drive vehicles and control mechanisms have not been conducted.

Overdosage

In clinical studies, there are no cases of overdose of the drug Prolia.
In clinical studies, doses of denosumab were administered up to 180> mg every 4 weeks (cumulative dose up to 1080 mg at 6 months).

  • Brand name: Prolia®
  • Active ingredient: Denosumab
  • Dosage form: Subcutaneous solution.
  • Manufacturer: Amgen Manewackering Limited
  • Country of Origin: USA

Studies and clinical trials of Denosumab (Click to expand)

  1. Denosumab-mediated increase in hand bone mineral density associated with decreased progression of bone erosion in rheumatoid arthritis patients
  2. An open-label, phase 2 trial of denosumab in the treatment of relapsed or plateau-phase multiple myeloma
  3. Denosumab treatment effects on structural damage, bone mineral density, and bone turnover in rheumatoid arthritis: A twelve-month, multicenter, randomized, double-blind, placebo-controlled, phase II clinical trial
  4. Integrated model for denosumab and ibandronate pharmacodynamics in postmenopausal women
  5. Relationship between bone mineral density changes with denosumab treatment and risk reduction for vertebral and nonvertebral fractures
  6. Five years of denosumab exposure in women with postmenopausal osteoporosis: Results from the first two years of the FREEDOM extension
  7. Effects of denosumab on bone histomorphometry: The FREEDOM and STAND studies
  8. Effects of denosumab on bone turnover markers in postmenopausal osteoporosis
  9. Effects of denosumab on fracture and bone mineral density by level of kidney function
  10. Bone remodeling in postmenopausal women who discontinued denosumab treatment: Off-treatment biopsy study
  11. Denosumab and changes in bone turnover markers during androgen deprivation therapy for prostate cancer
  12. Effect of denosumab treatment on the risk of fractures in subgroups of women with postmenopausal osteoporosis
  13. Preventing metastases to bone: Denosumab or bisphosphonates?
  14. Microarchitectural deterioration of cortical and trabecular bone: Differing effects of denosumab and alendronate
  15. Increased risk of serious infections in women with osteopenia or osteoporosis treated with denosumab
  16. Erratum to: Increased risk of serious infections in women with osteopenia or osteoporosis treated with denosumab
  17. Denosumab-related osteonecrosis of the jaws
  18. Do RANKL inhibitors (denosumab) affect inflammation and immunity?
  19. Erratum to: Do RANKL inhibitors (denosumab) affect inflammation and immunity?
  20. Adherence, preference, and satisfaction of postmenopausal women taking denosumab or alendronate
  21. Cost-effectiveness of Denosumab for the treatment of postmenopausal osteoporosis
  22. Infections in postmenopausal women with osteoporosis treated with denosumab or placebo: coincidence or causal association?
  23. Final results of the DAPS (Denosumab Adherence Preference Satisfaction) study: a 24-month, randomized, crossover comparison with alendronate in postmenopausal women
  24. Dose–response study of denosumab on bone mineral density and bone turnover markers in Japanese postmenopausal women with osteoporosis

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