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Primary Target

Hydroxyapatite

20

Histamine H1 receptor

316

Dopamine D2 receptor

311

DNA

282

Serotonin 2a (5-HT2a) receptor

237

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US Previously Marketed

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Investigational

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Approved

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Phase II

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Approval Year

1991

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1977

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Unknown

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Condition

Cancer-related hypercalcemia

12

Non-Hodgkin's lymphoma

12

Relapsed or refractory lymphoma

12

Heterotopic ossification

7

Paget’s disease of bone

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Treatment Modality

Primary

20

Preventing

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CNS Activity

CNS Penetrant

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CNS Non-penetrant

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Originator

Novartis

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Chemical

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CAS

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FDA UNII

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PUBCHEM

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EPA CompTox

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MERCK INDEX

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MUSCULO-SKELETAL SYSTEM

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DRUGS FOR TREATMENT OF BONE DISEASES

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ATC Level 3

DRUGS AFFECTING BONE STRUCTURE AND MINERALIZATION

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ATC Level 4

Bisphosphonates

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Bisphosphonates, combinations

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Salts, Hydrates, Esters, etc.

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Showing 1 - 10 of 20 results

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BECAMPANEL

X3D0O800AJ

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Status:

Investigational

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Glutamate receptor ionotropic AMPA

Conditions:

Becampanel (AMP397) is an aminomethylquinoxalinedione AMPA receptor antagonist. Also, AMP397 demonstrates binding to hydroxyapatite. AMP397 has no genotoxic potential in vivo. In particular, no genotoxic metabolite is formed in mammalian cells, and, ...

if formed by intestinal bacteria, is unable to exert any genotoxic activity in the adjacent intestinal tissue. AMP397 has a significant oral bioavailability of 22% in mice and approximately 50% in humans. It was under development for the potential treatment of status epilepticus and other types of seizures. However, this research has been discontinued. It is also being evaluated for use in the treatment of neuropathic pain and cerebrovascular ischemia.

GALLIUM CATION

F7K5MP217W

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Status:

US Previously Marketed

First approved in 1991

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Ribonucleoside-diphosphate reductase RR1

Serotransferrin

Ribonucleoside-diphosphate reductase RR1

Interleukin-1 beta

Conditions:

Non-Hodgkin's lymphoma

Relapsed or refractory lymphoma

Cancer-related hypercalcemia

Gallium nitrate (brand name Ganite) is a drug that is used to treat hyper-calcemia, or too much calcium in the blood. Ganite exerts a hypocalcemic effect by inhibiting calcium resorption from bone, possibly by reducing increased bone turnover. It was...

shown, that gallium favorably altered the mineral properties to enhance hydroxyapatite crystallization and reduced mineral solubility. The drug also acted on the cellular components of bone to reduce bone resorption by decreasing acid secretion by osteoclasts. Nevertheless, ganite was withdrawn from sale, although the reasons was not the safety or effectiveness. Gallium nitrate inhibits the growth of various lymphoma cell lines in vitro and exhibits antitumor activity in patients with lymphoma. Gallium binds avidly to the iron transport protein transferrin. Transferrin-gallium complexes preferentially target cells that express transferrin receptors on their surface. Expression of transferrin receptors is particularly high on lymphoma cells. Cellular uptake of the gallium-transferrin complex leads to inhibition of cellular proliferation primarily via disruption of iron transport and homeostasis and blockade of ribonucleotide reductase. In phase II of clinical trials in patients with relapsed or refractory lymphoma, the antitumor activity of gallium nitrate is similar to, or better than, that of other commonly used chemotherapeutic agents.

ETIDRONIC ACID

M2F465ROXU

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Status:

US Previously Marketed

First approved in 1977

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Conditions:

Heterotopic ossification

Paget’s disease of bone

Etidronate is a salt of etidronic acid (brand name Didronel, also known as EHDP) a diphosphonate, which is indicated for the treatment of symptomatic Paget’s disease of bone and in the prevention and treatment of heterotopic ossification following to...

tal hip replacement or due to spinal cord injury. Didronel is not approved for the treatment of osteoporosis. This drugs acts primarily on bone. It can inhibit the formation, growth, and dissolution of hydroxyapatite crystals and their amorphous precursors by chemisorption to calcium phosphate surfaces. Inhibition of crystal resorption occurs at lower doses than are required to inhibit crystal growth. Both effects increase as the dose increases. Preclinical studies indicate etidronate disodium does not cross the blood-brain barrier. Didronel is not metabolized. The amount of drug absorbed after an oral dose is approximately 3 percent. Bisphosphonates, when attached to bone tissue, are absorbed by osteoclasts, the bone cells that breaks down bone tissue. Although the mechanism of action of non-nitrogenous bisphosphonates has not been fully elucidated, available data suggest that they bind strongly to hydroxyapatite crystals in the bone matrix, preferentially at the sites of increased bone turnover and inhibit the formation and dissolution of the crystals. Other actions may include direct inhibition of mature osteoclast function, promotion of osteoclast apoptosis, and interference with osteoblast-mediated osteoclast activation. Etidronic acid may promote osteoclast apoptosis by competing with adenosine triphosphate (ATP) in the cellular energy metabolism. The osteoclast initiates apoptosis and dies, leading to an overall decrease in the breakdown of bone.

GALLIUM DICITRATE

6ZNH95J8XB

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Status:

US Previously Marketed

First approved in 1991

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Ribonucleoside-diphosphate reductase RR1

Serotransferrin

Ribonucleoside-diphosphate reductase RR1

Interleukin-1 beta

Conditions:

Non-Hodgkin's lymphoma

Relapsed or refractory lymphoma

Cancer-related hypercalcemia

Gallium nitrate (brand name Ganite) is a drug that is used to treat hyper-calcemia, or too much calcium in the blood. Ganite exerts a hypocalcemic effect by inhibiting calcium resorption from bone, possibly by reducing increased bone turnover. It was...

shown, that gallium favorably altered the mineral properties to enhance hydroxyapatite crystallization and reduced mineral solubility. The drug also acted on the cellular components of bone to reduce bone resorption by decreasing acid secretion by osteoclasts. Nevertheless, ganite was withdrawn from sale, although the reasons was not the safety or effectiveness. Gallium nitrate inhibits the growth of various lymphoma cell lines in vitro and exhibits antitumor activity in patients with lymphoma. Gallium binds avidly to the iron transport protein transferrin. Transferrin-gallium complexes preferentially target cells that express transferrin receptors on their surface. Expression of transferrin receptors is particularly high on lymphoma cells. Cellular uptake of the gallium-transferrin complex leads to inhibition of cellular proliferation primarily via disruption of iron transport and homeostasis and blockade of ribonucleotide reductase. In phase II of clinical trials in patients with relapsed or refractory lymphoma, the antitumor activity of gallium nitrate is similar to, or better than, that of other commonly used chemotherapeutic agents.

AMMONIUM HEXAFLUOROGALLATE

4X2AHU48WW

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Status:

US Previously Marketed

First approved in 1991

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Ribonucleoside-diphosphate reductase RR1

Serotransferrin

Ribonucleoside-diphosphate reductase RR1

Interleukin-1 beta

Conditions:

Non-Hodgkin's lymphoma

Relapsed or refractory lymphoma

Cancer-related hypercalcemia

Gallium nitrate (brand name Ganite) is a drug that is used to treat hyper-calcemia, or too much calcium in the blood. Ganite exerts a hypocalcemic effect by inhibiting calcium resorption from bone, possibly by reducing increased bone turnover. It was...

shown, that gallium favorably altered the mineral properties to enhance hydroxyapatite crystallization and reduced mineral solubility. The drug also acted on the cellular components of bone to reduce bone resorption by decreasing acid secretion by osteoclasts. Nevertheless, ganite was withdrawn from sale, although the reasons was not the safety or effectiveness. Gallium nitrate inhibits the growth of various lymphoma cell lines in vitro and exhibits antitumor activity in patients with lymphoma. Gallium binds avidly to the iron transport protein transferrin. Transferrin-gallium complexes preferentially target cells that express transferrin receptors on their surface. Expression of transferrin receptors is particularly high on lymphoma cells. Cellular uptake of the gallium-transferrin complex leads to inhibition of cellular proliferation primarily via disruption of iron transport and homeostasis and blockade of ribonucleotide reductase. In phase II of clinical trials in patients with relapsed or refractory lymphoma, the antitumor activity of gallium nitrate is similar to, or better than, that of other commonly used chemotherapeutic agents.

GALLIUM OXIDE

46F059V66A

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Status:

US Previously Marketed

First approved in 1991

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Ribonucleoside-diphosphate reductase RR1

Serotransferrin

Ribonucleoside-diphosphate reductase RR1

Interleukin-1 beta

Conditions:

Non-Hodgkin's lymphoma

Relapsed or refractory lymphoma

Cancer-related hypercalcemia

Gallium nitrate (brand name Ganite) is a drug that is used to treat hyper-calcemia, or too much calcium in the blood. Ganite exerts a hypocalcemic effect by inhibiting calcium resorption from bone, possibly by reducing increased bone turnover. It was...

shown, that gallium favorably altered the mineral properties to enhance hydroxyapatite crystallization and reduced mineral solubility. The drug also acted on the cellular components of bone to reduce bone resorption by decreasing acid secretion by osteoclasts. Nevertheless, ganite was withdrawn from sale, although the reasons was not the safety or effectiveness. Gallium nitrate inhibits the growth of various lymphoma cell lines in vitro and exhibits antitumor activity in patients with lymphoma. Gallium binds avidly to the iron transport protein transferrin. Transferrin-gallium complexes preferentially target cells that express transferrin receptors on their surface. Expression of transferrin receptors is particularly high on lymphoma cells. Cellular uptake of the gallium-transferrin complex leads to inhibition of cellular proliferation primarily via disruption of iron transport and homeostasis and blockade of ribonucleotide reductase. In phase II of clinical trials in patients with relapsed or refractory lymphoma, the antitumor activity of gallium nitrate is similar to, or better than, that of other commonly used chemotherapeutic agents.

GALLIUM NITRIDE (GAN)

1R9CC3P9VL

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Status:

US Previously Marketed

First approved in 1991

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Ribonucleoside-diphosphate reductase RR1

Serotransferrin

Ribonucleoside-diphosphate reductase RR1

Interleukin-1 beta

Conditions:

Non-Hodgkin's lymphoma

Relapsed or refractory lymphoma

Cancer-related hypercalcemia

Gallium nitrate (brand name Ganite) is a drug that is used to treat hyper-calcemia, or too much calcium in the blood. Ganite exerts a hypocalcemic effect by inhibiting calcium resorption from bone, possibly by reducing increased bone turnover. It was...

shown, that gallium favorably altered the mineral properties to enhance hydroxyapatite crystallization and reduced mineral solubility. The drug also acted on the cellular components of bone to reduce bone resorption by decreasing acid secretion by osteoclasts. Nevertheless, ganite was withdrawn from sale, although the reasons was not the safety or effectiveness. Gallium nitrate inhibits the growth of various lymphoma cell lines in vitro and exhibits antitumor activity in patients with lymphoma. Gallium binds avidly to the iron transport protein transferrin. Transferrin-gallium complexes preferentially target cells that express transferrin receptors on their surface. Expression of transferrin receptors is particularly high on lymphoma cells. Cellular uptake of the gallium-transferrin complex leads to inhibition of cellular proliferation primarily via disruption of iron transport and homeostasis and blockade of ribonucleotide reductase. In phase II of clinical trials in patients with relapsed or refractory lymphoma, the antitumor activity of gallium nitrate is similar to, or better than, that of other commonly used chemotherapeutic agents.

GALLIUM(III) HYDROXIDE

S3PJW60NUM

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Status:

US Previously Marketed

First approved in 1991

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Ribonucleoside-diphosphate reductase RR1

Serotransferrin

Ribonucleoside-diphosphate reductase RR1

Interleukin-1 beta

Conditions:

Non-Hodgkin's lymphoma

Relapsed or refractory lymphoma

Cancer-related hypercalcemia

Gallium nitrate (brand name Ganite) is a drug that is used to treat hyper-calcemia, or too much calcium in the blood. Ganite exerts a hypocalcemic effect by inhibiting calcium resorption from bone, possibly by reducing increased bone turnover. It was...

shown, that gallium favorably altered the mineral properties to enhance hydroxyapatite crystallization and reduced mineral solubility. The drug also acted on the cellular components of bone to reduce bone resorption by decreasing acid secretion by osteoclasts. Nevertheless, ganite was withdrawn from sale, although the reasons was not the safety or effectiveness. Gallium nitrate inhibits the growth of various lymphoma cell lines in vitro and exhibits antitumor activity in patients with lymphoma. Gallium binds avidly to the iron transport protein transferrin. Transferrin-gallium complexes preferentially target cells that express transferrin receptors on their surface. Expression of transferrin receptors is particularly high on lymphoma cells. Cellular uptake of the gallium-transferrin complex leads to inhibition of cellular proliferation primarily via disruption of iron transport and homeostasis and blockade of ribonucleotide reductase. In phase II of clinical trials in patients with relapsed or refractory lymphoma, the antitumor activity of gallium nitrate is similar to, or better than, that of other commonly used chemotherapeutic agents.

GALLIUM CITRATE

HT6C49L0ZP

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Status:

US Previously Marketed

First approved in 1991

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Ribonucleoside-diphosphate reductase RR1

Serotransferrin

Ribonucleoside-diphosphate reductase RR1

Interleukin-1 beta

Conditions:

Non-Hodgkin's lymphoma

Relapsed or refractory lymphoma

Cancer-related hypercalcemia

Gallium nitrate (brand name Ganite) is a drug that is used to treat hyper-calcemia, or too much calcium in the blood. Ganite exerts a hypocalcemic effect by inhibiting calcium resorption from bone, possibly by reducing increased bone turnover. It was...

shown, that gallium favorably altered the mineral properties to enhance hydroxyapatite crystallization and reduced mineral solubility. The drug also acted on the cellular components of bone to reduce bone resorption by decreasing acid secretion by osteoclasts. Nevertheless, ganite was withdrawn from sale, although the reasons was not the safety or effectiveness. Gallium nitrate inhibits the growth of various lymphoma cell lines in vitro and exhibits antitumor activity in patients with lymphoma. Gallium binds avidly to the iron transport protein transferrin. Transferrin-gallium complexes preferentially target cells that express transferrin receptors on their surface. Expression of transferrin receptors is particularly high on lymphoma cells. Cellular uptake of the gallium-transferrin complex leads to inhibition of cellular proliferation primarily via disruption of iron transport and homeostasis and blockade of ribonucleotide reductase. In phase II of clinical trials in patients with relapsed or refractory lymphoma, the antitumor activity of gallium nitrate is similar to, or better than, that of other commonly used chemotherapeutic agents.

GALLIUM TRIFLUORIDE

3EG50JLZ49

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Status:

US Previously Marketed

First approved in 1991

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Ribonucleoside-diphosphate reductase RR1

Serotransferrin

Ribonucleoside-diphosphate reductase RR1

Interleukin-1 beta

Conditions:

Non-Hodgkin's lymphoma

Relapsed or refractory lymphoma

Cancer-related hypercalcemia

Gallium nitrate (brand name Ganite) is a drug that is used to treat hyper-calcemia, or too much calcium in the blood. Ganite exerts a hypocalcemic effect by inhibiting calcium resorption from bone, possibly by reducing increased bone turnover. It was...

shown, that gallium favorably altered the mineral properties to enhance hydroxyapatite crystallization and reduced mineral solubility. The drug also acted on the cellular components of bone to reduce bone resorption by decreasing acid secretion by osteoclasts. Nevertheless, ganite was withdrawn from sale, although the reasons was not the safety or effectiveness. Gallium nitrate inhibits the growth of various lymphoma cell lines in vitro and exhibits antitumor activity in patients with lymphoma. Gallium binds avidly to the iron transport protein transferrin. Transferrin-gallium complexes preferentially target cells that express transferrin receptors on their surface. Expression of transferrin receptors is particularly high on lymphoma cells. Cellular uptake of the gallium-transferrin complex leads to inhibition of cellular proliferation primarily via disruption of iron transport and homeostasis and blockade of ribonucleotide reductase. In phase II of clinical trials in patients with relapsed or refractory lymphoma, the antitumor activity of gallium nitrate is similar to, or better than, that of other commonly used chemotherapeutic agents.

Showing 1 - 10 of 20 results

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