| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
Purity: ≥98%
| ln Vivo |
In a 6-year prospective study, postmenopausal osteoporotic women (n=60, mean age 62.3±7.5 years) received monthly intramuscular Neridronate 25 mg. Bone mineral density (BMD) increased significantly after 1 year at lumbar spine L1-L4 (mean change +4.5±0.9%, P≤0.05), total femur (+4.5±0.8%, P≤0.05), and femoral neck (+2.1±0.6%, P≤0.05). The increase at L1-L4 and total femur was maintained over 6 years; femoral neck BMD further improved up to year 3 and remained stable thereafter. [1]
Bone turnover biomarkers (CTX, NTX, osteocalcin, PTH, ionized calcium) progressively decreased over time (P≤0.05). CTX decreased by 61-66% at years 5-6, NTX by 46% at study end. Serum 25-hydroxyvitamin D increased significantly after 3 months (P≤0.001) and reached optimal levels (≥30 ng/mL) at year 1, maintained thereafter. Total calcium and bone alkaline phosphatase showed no significant changes. [1] No fractures and no significant adverse events were reported during the 6-year treatment. The dropout rate was 7%. [1] |
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| Toxicity/Toxicokinetics |
No significant adverse events were reported throughout the 6-year study period. No fractures occurred. [1]
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| References | |
| Additional Infomation |
Neridronate is a 1,1-bisphosphonate. It is a third-generation aminohexane bisphosphonate with anti-bone resorption and anti-hypercalcemic activity. Although its exact mechanism of action is not fully elucidated, neridronate binds to and adsorbs hydroxyapatite crystals in the bone matrix, thereby inhibiting osteoclast-mediated bone resorption. The drug also binds to and inhibits the activity of farnesyl pyrophosphate synthase, an enzyme that plays a crucial role in the mevalonate pathway. This inhibits the formation of isoprene compounds, which are substrates for protein isoprenelation. This prevents farnesylation and geraniylgeraniylation of proteins essential for osteoclast function, thereby inducing osteoclast apoptosis. By inhibiting osteoclast-mediated bone resorption, neridronate reduces bone turnover, stabilizes the bone matrix, and alleviates hypercalcemia.
Neridronate is a nitrogen-containing bisphosphonate. It is administered intramuscularly at 25 mg once monthly. In this study, 81.3% of patients received calcium and vitamin D supplementation to maintain 25-OH-D ≥30 ng/mL. A negative correlation was observed between 25-OH-D levels and CTX (r=-0.33, P≤0.0001) and NTX (r=-0.31, P≤0.0002). The study was approved by the Local Ethical Committee and registered at ClinicalTrials.gov (NCT03699150). [1] |
| Molecular Formula |
C6H17NO7P2
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|---|---|
| Molecular Weight |
277.14928
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| Exact Mass |
277.048
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| CAS # |
79778-41-9
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| Related CAS # |
80729-79-9 (sodium);79778-41-9 (free acid);
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| PubChem CID |
71237
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| Appearance |
White to off-white solid powder
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| Density |
1.7±0.1 g/cm3
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| Boiling Point |
600.1±65.0 °C at 760 mmHg
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| Melting Point |
245°
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| Flash Point |
316.7±34.3 °C
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| Vapour Pressure |
0.0±3.9 mmHg at 25°C
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| Index of Refraction |
1.569
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| LogP |
-3.36
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
16
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| Complexity |
286
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=P(C(P(O)(O)=O)(CCCCCN)O)(O)O
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| InChi Key |
PUUSSSIBPPTKTP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C6H17NO7P2/c7-5-3-1-2-4-6(8,15(9,10)11)16(12,13)14/h8H,1-5,7H2,(H2,9,10,11)(H2,12,13,14)
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| Chemical Name |
(6-Amino-1-hydroxyhexylidene)diphosphonic acid
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| Synonyms |
Neridronic acid; Nerixia.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~5 mg/mL (~18.04 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2 mg/mL (7.22 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C).
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6082 mL | 18.0408 mL | 36.0815 mL | |
| 5 mM | 0.7216 mL | 3.6082 mL | 7.2163 mL | |
| 10 mM | 0.3608 mL | 1.8041 mL | 3.6082 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01803360 | UNKNOWN STATUS | Drug: Neridronate | Osteoarthritis, Knee | ASST Gaetano Pini-CTO | 2013-03 | Phase 2 |
| NCT01140321 | COMPLETED | Drug: Neridronate | Osteoporosis Thalassemia Intermedia Thalassemia Major |
Ente Ospedaliero Ospedali Galliera | 2004-01 | Phase 2 |
| NCT02402530 | COMPLETED | Drug: Placebo Drug: Neridronic acid 62.5 mg |
Complex Regional Pain Syndrome, Type I | Grünenthal GmbH | 2015-04 | Phase 2 Phase 3 |
| NCT02972359 | COMPLETEDWITH RESULTS | Drug: Neridronic acid | Complex Regional Pain Syndrome | Grünenthal GmbH | 2016-12-20 | Phase 3 |
| NCT03560986 | TERMINATEDWITH RESULTS | Drug: Neridronic acid 100 mg Drug: Placebo |
Complex Regional Pain Syndrome (CRPS) | Grünenthal GmbH | 2018-05-31 | Phase 3 |
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