Ranelic Acid

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Sohita Dhillon - One of the best experts on this subject based on the ideXlab platform.

  • Spotlight on Strontium Ranelate
    Drugs & Aging, 2010
    Co-Authors: Emma D. Deeks, Sohita Dhillon
    Abstract:

    This is a review of the pharmacology of strontium ranelate (Protelos®, Protos®, Protaxos®, Bivalos®, Osseor®), and its efficacy and tolerability in the treatment of patients with postmenopausal osteoporosis. Strontium ranelate is a divalent strontium salt of Ranelic Acid that is capable of increasing bone formation and reducing bone resorption, thereby uncoupling and rebalancing bone turnover in favour of bone formation. The drug is effective in reducing the risk of fractures, including both vertebral and nonvertebral fractures, in patients with postmenopausal osteoporosis, according to data from two large, double-blind, placebo-controlled, multicentre trials of 5 years’ duration, and reduced the risk of hip fracture in high-risk patients in a post hoc analysis of one trial. Moreover, data from patients who continued to receive the drug during the 3-year extension phase of these trials indicate that strontium ranelate continues to provide protection against new vertebral fractures and nonvertebral fractures for up to 8 years of therapy. It also improves bone mineral density at numerous sites and both increases markers of bone formation and decreases markers of bone resorption. Strontium ranelate is administered orally as a suspension and is generally well tolerated. The nature of adverse events was generally similar regardless of treatment duration in clinical trials, with the most commonly reported being nausea and diarrhoea over 5 years of treatment, and memory loss and diarrhoea during longer-term treatment. Although an increased risk of venous thromboembolism was associated with strontium ranelate relative to placebo over 5 years of treatment in a pooled analysis of clinical trials, postmarketing data have not confirmed this finding. Overall, the clinical data available suggest that strontium ranelate is an effective and generally well tolerated option for the first-line treatment of postmenopausal osteoporosis.

  • Spotlight on strontium ranelate: in postmenopausal osteoporosis.
    Drugs & aging, 2010
    Co-Authors: Emma D. Deeks, Sohita Dhillon
    Abstract:

    This is a review of the pharmacology of strontium ranelate (Protelos®, Protos®, Protaxos®, Bivalos®, Osseor®), and its efficacy and tolerability in the treatment of patients with postmenopausal osteoporosis. Strontium ranelate is a divalent strontium salt of Ranelic Acid that is capable of increasing bone formation and reducing bone resorption, thereby uncoupling and rebalancing bone turnover in favour of bone formation. The drug is effective in reducing the risk of fractures, including both vertebral and nonvertebral fractures, in patients with postmenopausal osteoporosis, according to data from two large, double-blind, placebo-controlled, multicentre trials of 5 years’ duration, and reduced the risk of hip fracture in high-risk patients in a post hoc analysis of one trial. Moreover, data from patients who continued to receive the drug during the 3-year extension phase of these trials indicate that strontium ranelate continues to provide protection against new vertebral fractures and nonvertebral fractures for up to 8 years of therapy. It also improves bone mineral density at numerous sites and both increases markers of bone formation and decreases markers of bone resorption. Strontium ranelate is administered orally as a suspension and is generally well tolerated. The nature of adverse events was generally similar regardless of treatment duration in clinical trials, with the most commonly reported being nausea and diarrhoea over 5 years of treatment, and memory loss and diarrhoea during longer-term treatment. Although an increased risk of venous thromboembolism was associated with strontium ranelate relative to placebo over 5 years of treatment in a pooled analysis of clinical trials, postmarketing data have not confirmed this finding. Overall, the clinical data available suggest that strontium ranelate is an effective and generally well tolerated option for the first-line treatment of postmenopausal osteoporosis.

  • Strontium ranelate: a review of its use in the treatment of postmenopausal osteoporosis.
    Drugs, 2010
    Co-Authors: Emma D. Deeks, Sohita Dhillon
    Abstract:

    This is a review of the pharmacology of strontium ranelate (Protelos, Protos, Protaxos, Bivalos, Osseor), and its efficacy and tolerability in the treatment of patients with postmenopausal osteoporosis. Strontium ranelate is a divalent strontium salt of Ranelic Acid that is capable of increasing bone formation and reducing bone resorption, thereby uncoupling and rebalancing bone turnover in favour of bone formation. The drug is effective in reducing the risk of fractures, including both vertebral and nonvertebral fractures, in patients with postmenopausal osteoporosis, according to data from two large, double-blind, placebo-controlled, multicentre trials of 5 years' duration, and reduced the risk of hip fracture in high-risk patients in a post hoc analysis of one trial. Moreover, data from patients who continued to receive the drug during the 3-year extension phases of these trials indicate that strontium ranelate continues to provide protection against new vertebral fractures and nonvertebral fractures for up to 8 years of therapy. It also improves bone mineral density at numerous sites and both increases markers of bone formation and decreases markers of bone resorption. Strontium ranelate is administered orally as a suspension and is generally well tolerated. The nature of adverse events was generally similar regardless of treatment duration in clinical trials, with the most commonly reported being nausea and diarrhoea over 5 years of treatment, and memory loss and diarrhoea during longer-term treatment. Although an increased risk of venous thromboembolism was associated with strontium ranelate relative to placebo over 5 years of treatment in a pooled analysis of clinical trials, postmarketing data have not confirmed this finding. Overall, the clinical data available suggest that strontium ranelate is an effective and generally well tolerated option for the first-line treatment of postmenopausal osteoporosis.

  • Strontium Ranelate
    Drugs, 2010
    Co-Authors: Emma D. Deeks, Sohita Dhillon
    Abstract:

    This is a review of the pharmacology of strontium ranelate (Protelos®, Protos®, Protaxos®, Bivalos®, Osseor®), and its efficacy and tolerability in the treatment of patients with postmenopausal osteoporosis. Strontium ranelate is a divalent strontium salt of Ranelic Acid that is capable of increasing bone formation and reducing bone resorption, thereby uncoupling and rebalancing bone turnover in favour of bone formation. The drug is effective in reducing the risk of fractures, including both vertebral and nonvertebral fractures, in patients with postmenopausal osteoporosis, according to data from two large, double-blind, placebo-controlled, multicentre trials of 5 years’ duration, and reduced the risk of hip fracture in high-risk patients in a post hoc analysis of one trial. Moreover, data from patients who continued to receive the drug during the 3-year extension phases of these trials indicate that strontium ranelate continues to provide protection against new vertebral fractures and nonvertebral fractures for up to 8 years of therapy. It also improves bone mineral density at numerous sites and both increases markers of bone formation and decreases markers of bone resorption. Strontium ranelate is administered orally as a suspension and is generally well tolerated. The nature of adverse events was generally similar regardless of treatment duration in clinical trials, with the most commonly reported being nausea and diarrhoea over 5 years of treatment, and memory loss and diarrhoea during longer-term treatment. Although an increased risk of venous thromboembolism was associated with strontium ranelate relative to placebo over 5 years of treatment in a pooled analysis of clinical trials, postmarketing data have not confirmed this finding. Overall, the clinical data available suggest that strontium ranelate is an effective and generally well tolerated option for the first-line treatment of postmenopausal osteoporosis.

Begoña Ferrari - One of the best experts on this subject based on the ideXlab platform.

  • Effect of SrR delivery in the biomarkers of bone regeneration during the in vitro degradation of HNT/GN coatings prepared by EPD
    Colloids and surfaces. B Biointerfaces, 2020
    Co-Authors: Seyyed Behnam Abdollahi Boraei, Jhamak Nourmohammadi, Fatemeh Sadat Mahdavi, J. Yus, Ana Ferrández-montero, Antonio Javier Sanchez-herencia, Zoilo Gonzalez, Begoña Ferrari
    Abstract:

    Among strontium-based drugs, the Strontium ranelate (SrR) is a divalent strontium salt of Ranelic Acid which has an overall effect over the bone microarchitecture improvement. However, some findings reveal that the SrR affects in an opposite manner to the cell proliferation and osteoblastic differentiation, based on its concentration. Consequently, its release should be controlled. The incorporation of Halloysite nanotubes (HNT) as nanocarriers of SrR, into gelatine (GN) coatings, tailors the release of this anabolic bone-forming and anti-catabolic agent to stimulate bone growth. In fact, as-prepared GN/HNT-SrR coatings release 100 % SrR in phosphate buffered saline (PBS) within 21 days, and cellular studies of the nanocomposite coatings (MTT, Alkaline Phosphatase activity (ALP) and Calcium deposition assay) confirm the valuable bio-performance of these composite coatings to enhanced bone regeneration. In the present manuscript, suspensions with HNT/GN weight ratio of 0.5 are formulated to coat AISI 316 L stainless steel foils by Electrophoretic Deposition (EPD). Zeta potential determination is used to stablish the drug loading (HNT-SrR) by electrostatic interaction, as well as to optimize the dispersion of bare HNT and HNT SrR-loaded in a GN aqueous solution. Polyethilenimnine (PEI) is used as stabilizer to buffer the suspension media, assure cargo-drug dispersion and sequential release, while the thermal gelling of the suspension controls and step up the coating formation during EPD.

Emma D. Deeks - One of the best experts on this subject based on the ideXlab platform.

  • Spotlight on Strontium Ranelate
    Drugs & Aging, 2010
    Co-Authors: Emma D. Deeks, Sohita Dhillon
    Abstract:

    This is a review of the pharmacology of strontium ranelate (Protelos®, Protos®, Protaxos®, Bivalos®, Osseor®), and its efficacy and tolerability in the treatment of patients with postmenopausal osteoporosis. Strontium ranelate is a divalent strontium salt of Ranelic Acid that is capable of increasing bone formation and reducing bone resorption, thereby uncoupling and rebalancing bone turnover in favour of bone formation. The drug is effective in reducing the risk of fractures, including both vertebral and nonvertebral fractures, in patients with postmenopausal osteoporosis, according to data from two large, double-blind, placebo-controlled, multicentre trials of 5 years’ duration, and reduced the risk of hip fracture in high-risk patients in a post hoc analysis of one trial. Moreover, data from patients who continued to receive the drug during the 3-year extension phase of these trials indicate that strontium ranelate continues to provide protection against new vertebral fractures and nonvertebral fractures for up to 8 years of therapy. It also improves bone mineral density at numerous sites and both increases markers of bone formation and decreases markers of bone resorption. Strontium ranelate is administered orally as a suspension and is generally well tolerated. The nature of adverse events was generally similar regardless of treatment duration in clinical trials, with the most commonly reported being nausea and diarrhoea over 5 years of treatment, and memory loss and diarrhoea during longer-term treatment. Although an increased risk of venous thromboembolism was associated with strontium ranelate relative to placebo over 5 years of treatment in a pooled analysis of clinical trials, postmarketing data have not confirmed this finding. Overall, the clinical data available suggest that strontium ranelate is an effective and generally well tolerated option for the first-line treatment of postmenopausal osteoporosis.

  • Spotlight on strontium ranelate: in postmenopausal osteoporosis.
    Drugs & aging, 2010
    Co-Authors: Emma D. Deeks, Sohita Dhillon
    Abstract:

    This is a review of the pharmacology of strontium ranelate (Protelos®, Protos®, Protaxos®, Bivalos®, Osseor®), and its efficacy and tolerability in the treatment of patients with postmenopausal osteoporosis. Strontium ranelate is a divalent strontium salt of Ranelic Acid that is capable of increasing bone formation and reducing bone resorption, thereby uncoupling and rebalancing bone turnover in favour of bone formation. The drug is effective in reducing the risk of fractures, including both vertebral and nonvertebral fractures, in patients with postmenopausal osteoporosis, according to data from two large, double-blind, placebo-controlled, multicentre trials of 5 years’ duration, and reduced the risk of hip fracture in high-risk patients in a post hoc analysis of one trial. Moreover, data from patients who continued to receive the drug during the 3-year extension phase of these trials indicate that strontium ranelate continues to provide protection against new vertebral fractures and nonvertebral fractures for up to 8 years of therapy. It also improves bone mineral density at numerous sites and both increases markers of bone formation and decreases markers of bone resorption. Strontium ranelate is administered orally as a suspension and is generally well tolerated. The nature of adverse events was generally similar regardless of treatment duration in clinical trials, with the most commonly reported being nausea and diarrhoea over 5 years of treatment, and memory loss and diarrhoea during longer-term treatment. Although an increased risk of venous thromboembolism was associated with strontium ranelate relative to placebo over 5 years of treatment in a pooled analysis of clinical trials, postmarketing data have not confirmed this finding. Overall, the clinical data available suggest that strontium ranelate is an effective and generally well tolerated option for the first-line treatment of postmenopausal osteoporosis.

  • Strontium ranelate: a review of its use in the treatment of postmenopausal osteoporosis.
    Drugs, 2010
    Co-Authors: Emma D. Deeks, Sohita Dhillon
    Abstract:

    This is a review of the pharmacology of strontium ranelate (Protelos, Protos, Protaxos, Bivalos, Osseor), and its efficacy and tolerability in the treatment of patients with postmenopausal osteoporosis. Strontium ranelate is a divalent strontium salt of Ranelic Acid that is capable of increasing bone formation and reducing bone resorption, thereby uncoupling and rebalancing bone turnover in favour of bone formation. The drug is effective in reducing the risk of fractures, including both vertebral and nonvertebral fractures, in patients with postmenopausal osteoporosis, according to data from two large, double-blind, placebo-controlled, multicentre trials of 5 years' duration, and reduced the risk of hip fracture in high-risk patients in a post hoc analysis of one trial. Moreover, data from patients who continued to receive the drug during the 3-year extension phases of these trials indicate that strontium ranelate continues to provide protection against new vertebral fractures and nonvertebral fractures for up to 8 years of therapy. It also improves bone mineral density at numerous sites and both increases markers of bone formation and decreases markers of bone resorption. Strontium ranelate is administered orally as a suspension and is generally well tolerated. The nature of adverse events was generally similar regardless of treatment duration in clinical trials, with the most commonly reported being nausea and diarrhoea over 5 years of treatment, and memory loss and diarrhoea during longer-term treatment. Although an increased risk of venous thromboembolism was associated with strontium ranelate relative to placebo over 5 years of treatment in a pooled analysis of clinical trials, postmarketing data have not confirmed this finding. Overall, the clinical data available suggest that strontium ranelate is an effective and generally well tolerated option for the first-line treatment of postmenopausal osteoporosis.

  • Strontium Ranelate
    Drugs, 2010
    Co-Authors: Emma D. Deeks, Sohita Dhillon
    Abstract:

    This is a review of the pharmacology of strontium ranelate (Protelos®, Protos®, Protaxos®, Bivalos®, Osseor®), and its efficacy and tolerability in the treatment of patients with postmenopausal osteoporosis. Strontium ranelate is a divalent strontium salt of Ranelic Acid that is capable of increasing bone formation and reducing bone resorption, thereby uncoupling and rebalancing bone turnover in favour of bone formation. The drug is effective in reducing the risk of fractures, including both vertebral and nonvertebral fractures, in patients with postmenopausal osteoporosis, according to data from two large, double-blind, placebo-controlled, multicentre trials of 5 years’ duration, and reduced the risk of hip fracture in high-risk patients in a post hoc analysis of one trial. Moreover, data from patients who continued to receive the drug during the 3-year extension phases of these trials indicate that strontium ranelate continues to provide protection against new vertebral fractures and nonvertebral fractures for up to 8 years of therapy. It also improves bone mineral density at numerous sites and both increases markers of bone formation and decreases markers of bone resorption. Strontium ranelate is administered orally as a suspension and is generally well tolerated. The nature of adverse events was generally similar regardless of treatment duration in clinical trials, with the most commonly reported being nausea and diarrhoea over 5 years of treatment, and memory loss and diarrhoea during longer-term treatment. Although an increased risk of venous thromboembolism was associated with strontium ranelate relative to placebo over 5 years of treatment in a pooled analysis of clinical trials, postmarketing data have not confirmed this finding. Overall, the clinical data available suggest that strontium ranelate is an effective and generally well tolerated option for the first-line treatment of postmenopausal osteoporosis.

Hongtao Wei - One of the best experts on this subject based on the ideXlab platform.

  • the ethyl tetra ester of Ranelic Acid
    Acta Crystallographica Section E-structure Reports Online, 2007
    Co-Authors: Hongtao Wei
    Abstract:

    The title compound, 5-[bis­(ethoxy­carbonyl­meth­yl)amino]-4-cyano-2-ethoxy­carbonyl-3-thio­phene­propionate, C20H26N2O8S, is a highly substituted thio­phene ring with a crystal structure stabilized by inter­molecular C—H⋯O hydrogen bonds, which are, however, weak in strength.

  • The ethyl tetra­ester of Ranelic Acid
    Acta Crystallographica Section E Structure Reports Online, 2007
    Co-Authors: Hongtao Wei
    Abstract:

    The title compound, 5-[bis­(ethoxy­carbonyl­meth­yl)amino]-4-cyano-2-ethoxy­carbonyl-3-thio­phene­propionate, C20H26N2O8S, is a highly substituted thio­phene ring with a crystal structure stabilized by inter­molecular C—H⋯O hydrogen bonds, which are, however, weak in strength.

Seyyed Behnam Abdollahi Boraei - One of the best experts on this subject based on the ideXlab platform.

  • Effect of SrR delivery in the biomarkers of bone regeneration during the in vitro degradation of HNT/GN coatings prepared by EPD
    Colloids and surfaces. B Biointerfaces, 2020
    Co-Authors: Seyyed Behnam Abdollahi Boraei, Jhamak Nourmohammadi, Fatemeh Sadat Mahdavi, J. Yus, Ana Ferrández-montero, Antonio Javier Sanchez-herencia, Zoilo Gonzalez, Begoña Ferrari
    Abstract:

    Among strontium-based drugs, the Strontium ranelate (SrR) is a divalent strontium salt of Ranelic Acid which has an overall effect over the bone microarchitecture improvement. However, some findings reveal that the SrR affects in an opposite manner to the cell proliferation and osteoblastic differentiation, based on its concentration. Consequently, its release should be controlled. The incorporation of Halloysite nanotubes (HNT) as nanocarriers of SrR, into gelatine (GN) coatings, tailors the release of this anabolic bone-forming and anti-catabolic agent to stimulate bone growth. In fact, as-prepared GN/HNT-SrR coatings release 100 % SrR in phosphate buffered saline (PBS) within 21 days, and cellular studies of the nanocomposite coatings (MTT, Alkaline Phosphatase activity (ALP) and Calcium deposition assay) confirm the valuable bio-performance of these composite coatings to enhanced bone regeneration. In the present manuscript, suspensions with HNT/GN weight ratio of 0.5 are formulated to coat AISI 316 L stainless steel foils by Electrophoretic Deposition (EPD). Zeta potential determination is used to stablish the drug loading (HNT-SrR) by electrostatic interaction, as well as to optimize the dispersion of bare HNT and HNT SrR-loaded in a GN aqueous solution. Polyethilenimnine (PEI) is used as stabilizer to buffer the suspension media, assure cargo-drug dispersion and sequential release, while the thermal gelling of the suspension controls and step up the coating formation during EPD.