Page last updated: 2024-12-08

1-hydroxypentane-1,1-bisphosphonate

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

1-hydroxypentane-1,1-bisphosphonate is a **synthetic analogue of pyrophosphate** and is a potent inhibitor of **bone resorption**. It's not a common name, and you might find it referred to by other names like:

* **Pamidronate**
* **Aredia** (trade name)

**Here's why it's important for research:**

* **Osteoporosis Treatment:** Pamidronate is a medication used to treat osteoporosis, Paget's disease, and other bone diseases. It works by reducing bone breakdown and stimulating new bone formation.
* **Cancer Treatment:** Pamidronate is also used to treat hypercalcemia (high calcium levels in the blood) associated with some cancers. It can also be used to prevent bone complications in patients with multiple myeloma and breast cancer.
* **Research Tool:** As a potent inhibitor of bone resorption, pamidronate is a valuable research tool for studying bone metabolism and the development of new drugs for osteoporosis and other bone disorders.

**Mechanism of Action:**

Pamidronate works by:

* **Inhibiting farnesyl pyrophosphate synthase (FPPS):** This enzyme is critical for the production of isoprenoids, which are essential for the function of osteoclasts (the cells responsible for bone breakdown).
* **Interfering with osteoclast activity:** Pamidronate inhibits osteoclast formation and activity, leading to reduced bone resorption.

**Research Focus:**

* **Developing New Bone Resorption Inhibitors:** Pamidronate and other bisphosphonates serve as a foundation for developing new drugs with improved efficacy and fewer side effects.
* **Understanding Bone Metabolism:** Research using pamidronate helps scientists understand the complex mechanisms involved in bone formation and breakdown.
* **Developing New Therapies for Bone Diseases:** Research is ongoing to explore new applications for pamidronate and other bisphosphonates, such as in the treatment of bone infections and bone tumors.

**In summary, 1-hydroxypentane-1,1-bisphosphonate (Pamidronate) is a valuable tool for research and treatment, helping scientists understand bone metabolism and develop new therapies for a variety of bone disorders.**

Cross-References

ID SourceID
PubMed CID405378
CHEMBL ID299491
SCHEMBL ID4093004
MeSH IDM0155638

Synonyms (12)

Synonym
phosphonic acid, (1-hydroxypentylidene)bis-
(1-hydroxy-1-phosphono-pentyl)phosphonic acid
hpebp
CHEMBL299491 ,
1-hydroxy-pentane-1,1-bisphosphonate
1-hydroxypentane-1,1-diyldiphosphonic acid
bdbm50098379
(1-hydroxy-1-phosphono-pentyl)-phosphonic acid
57638-03-6
1-hydroxypentane-1,1-bisphosphonate
SCHEMBL4093004
DTXSID10206314
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Geranylgeranyl pyrophosphate synthaseHomo sapiens (human)IC50 (µMol)200.00000.00401.02764.5000AID74507
Farnesyl pyrophosphate synthase Leishmania donovaniIC50 (µMol)100.00000.11000.15600.1700AID72651
HTrypanosoma bruceiIC50 (µMol)12.70002.10002.10002.1000AID254970
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (5)

Processvia Protein(s)Taxonomy
isoprenoid metabolic processGeranylgeranyl pyrophosphate synthaseHomo sapiens (human)
geranyl diphosphate biosynthetic processGeranylgeranyl pyrophosphate synthaseHomo sapiens (human)
geranylgeranyl diphosphate biosynthetic processGeranylgeranyl pyrophosphate synthaseHomo sapiens (human)
farnesyl diphosphate biosynthetic processGeranylgeranyl pyrophosphate synthaseHomo sapiens (human)
isoprenoid biosynthetic processGeranylgeranyl pyrophosphate synthaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (7)

Processvia Protein(s)Taxonomy
dimethylallyltranstransferase activityGeranylgeranyl pyrophosphate synthaseHomo sapiens (human)
farnesyltranstransferase activityGeranylgeranyl pyrophosphate synthaseHomo sapiens (human)
geranyltranstransferase activityGeranylgeranyl pyrophosphate synthaseHomo sapiens (human)
protein bindingGeranylgeranyl pyrophosphate synthaseHomo sapiens (human)
identical protein bindingGeranylgeranyl pyrophosphate synthaseHomo sapiens (human)
metal ion bindingGeranylgeranyl pyrophosphate synthaseHomo sapiens (human)
prenyltransferase activityGeranylgeranyl pyrophosphate synthaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (5)

Processvia Protein(s)Taxonomy
nucleoplasmGeranylgeranyl pyrophosphate synthaseHomo sapiens (human)
cytoplasmGeranylgeranyl pyrophosphate synthaseHomo sapiens (human)
cytosolGeranylgeranyl pyrophosphate synthaseHomo sapiens (human)
Z discGeranylgeranyl pyrophosphate synthaseHomo sapiens (human)
perinuclear region of cytoplasmGeranylgeranyl pyrophosphate synthaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (23)

Assay IDTitleYearJournalArticle
AID96034Toxicity evaluated against human nasopharyngeal carcinoma KB cell line2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
Effects of bisphosphonates on the growth of Entamoeba histolytica and Plasmodium species in vitro and in vivo.
AID235219Therapeutic index measured as the ratio of LD50 (KB cells) to IC50 (T.b. rhodesiense)2002Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
Activity of bisphosphonates against Trypanosoma brucei rhodesiense.
AID249161Lethal dose required to inhibit the growth of human KB (nasopharyngeal carcinoma) cell line2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Bisphosphonate inhibitors of Toxoplasma gondi growth: in vitro, QSAR, and in vivo investigations.
AID151353Inhibition of Plasmodium falciparum 3D7 in erythrocytes2001Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6
Bisphosphonates inhibit the growth of Trypanosoma brucei, Trypanosoma cruzi, Leishmania donovani, Toxoplasma gondii, and Plasmodium falciparum: a potential route to chemotherapy.
AID208217Predicted pIC50 against Trypomastigotes Brucei rhodesiense.2002Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
Activity of bisphosphonates against Trypanosoma brucei rhodesiense.
AID208225Inhibition of Trypanosoma rhodesiense (strain STIB900) was determined using blood stream from trypomastigotes2001Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6
Bisphosphonates inhibit the growth of Trypanosoma brucei, Trypanosoma cruzi, Leishmania donovani, Toxoplasma gondii, and Plasmodium falciparum: a potential route to chemotherapy.
AID95764Inhibition of L. donovani (Amastigotes) strain MHOM/ET/67/L82 maintained in female golden hamsters2001Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6
Bisphosphonates inhibit the growth of Trypanosoma brucei, Trypanosoma cruzi, Leishmania donovani, Toxoplasma gondii, and Plasmodium falciparum: a potential route to chemotherapy.
AID254970Inhibition of recombinant Trypanosoma brucei soluble vacuolar pyrophosphatase expressed in Escherichia coli2005Journal of medicinal chemistry, Sep-22, Volume: 48, Issue:19
Bisphosphonate inhibition of the exopolyphosphatase activity of the Trypanosoma brucei soluble vacuolar pyrophosphatase.
AID9382850% lethal dose for inhibition of KB cells growth2002Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
Activity of bisphosphonates against Trypanosoma brucei rhodesiense.
AID74507Inhibitory activity against the human recombinant geranylgeranyl diphosphate synthase (GGPPSase).2002Journal of medicinal chemistry, May-23, Volume: 45, Issue:11
Inhibition of geranylgeranyl diphosphate synthase by bisphosphonates and diphosphates: a potential route to new bone antiresorption and antiparasitic agents.
AID208084In vitro growth inhibition of bloodstream-form Trypanosoma brucei rhodesiense Trypomastigotes2002Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
Activity of bisphosphonates against Trypanosoma brucei rhodesiense.
AID256540Dose to inhibit the growth of human KB carcinoma cell line2005Journal of medicinal chemistry, Sep-22, Volume: 48, Issue:19
Bisphosphonate inhibition of the exopolyphosphatase activity of the Trypanosoma brucei soluble vacuolar pyrophosphatase.
AID248772In vitro inhibitory concentration against the growth of Toxoplasma gondii in human foreskin fibroblast monolayer cells (HFF cells)2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Bisphosphonate inhibitors of Toxoplasma gondi growth: in vitro, QSAR, and in vivo investigations.
AID496826Antimicrobial activity against Entamoeba histolytica2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID244679Therapeutic index (TI) value as ratio of lethal dose (LD50) to the inhibitory concentration (IC50)2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Bisphosphonate inhibitors of Toxoplasma gondi growth: in vitro, QSAR, and in vivo investigations.
AID214469Inhibition of Trypanosoma cruzi Amastigotes was determined in Vero cells culture and fetal calf serum2001Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6
Bisphosphonates inhibit the growth of Trypanosoma brucei, Trypanosoma cruzi, Leishmania donovani, Toxoplasma gondii, and Plasmodium falciparum: a potential route to chemotherapy.
AID67525In vitro growth inhibition against Entamoeba histolytica2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
Effects of bisphosphonates on the growth of Entamoeba histolytica and Plasmodium species in vitro and in vivo.
AID72651Inhibitory activity against Leishmania major Farnesyl diphosphate synthase2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
Effects of bisphosphonates on the growth of Entamoeba histolytica and Plasmodium species in vitro and in vivo.
AID496819Antimicrobial activity against Plasmodium falciparum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID235248Therapeutic index was expressed as ratio of LD50 for KB cell line to IC50 against Plasmodium falciparum2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
Effects of bisphosphonates on the growth of Entamoeba histolytica and Plasmodium species in vitro and in vivo.
AID255448Ratio of ED50 against KB cell line to that of IC50 of TbVSP12005Journal of medicinal chemistry, Sep-22, Volume: 48, Issue:19
Bisphosphonate inhibition of the exopolyphosphatase activity of the Trypanosoma brucei soluble vacuolar pyrophosphatase.
AID275054Antibacterial activity against Escherichia coli W31102006Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25
Isoprenoid biosynthesis as a drug target: bisphosphonate inhibition of Escherichia coli K12 growth and synergistic effects of fosmidomycin.
AID158550In vitro growth inhibition against Plasmodium falciparum2004Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
Effects of bisphosphonates on the growth of Entamoeba histolytica and Plasmodium species in vitro and in vivo.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (9)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901 (11.11)18.7374
1990's0 (0.00)18.2507
2000's7 (77.78)29.6817
2010's1 (11.11)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.83

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index11.83 (24.57)
Research Supply Index2.30 (2.92)
Research Growth Index4.14 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.83)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other9 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]