bisphosphonate

Digeranyl bisphosphonate (DGBP) is a potent geranylgeranyl pyrophosphate (GGPP) synthase inhibitor that impedes the geranyl pyrophosphorylation of Rac1 and induces autophagy without causing apoptosis.

Aminobutane bisphosphonate is a powerful inhibitor of bone resorption. It can potentially be a useful measure for controlling hypercalcemia in patients with carcinoma.

Alendronate sodium hydrate (MK 217) is a nitrogen-containing bisphosphonate, which is an effective inhibitor of bone resorption. It is utilized for the treatment and prevention of osteoporosis.

Zoledronic Acid (ZOL 446) is a bisphosphonate. Zoledronic Acid (ZOL 446) is used to prevent skeletal fractures in patients with cancers such as multiple myeloma and prostate cancer. It can also be used to treat hypercalcemia of malignancy and can be helpful for treating pain from bone metastases. An annual dose of Zoledronate may also prevent recurring fractures in patients with a previous hip fracture. Zoledronic Acid (ZOL 446) is a single 5 mg infusion for the treatment of Paget's disease of bone. In 2007, the FDA also approved Reclast for the treatment of postmenopausal osteoporosis.

Ibandronate sodium (Boniva) is a synthetic nitrogen-containing bisphosphonate, used for the treatment of osteoporosis.

Zoledronic acid monohydrate (CGP 42446) is a synthetic imidazole bisphosphonate analog with anti-bone-resorption activity.

Medronic acid (Methylenediphosphonic acid), a methylene-substituted bisphosphonate, exhibits affinity for and adherence to hydroxyapatite crystals within the bone matrix. Accumulating at sites of osteoid mineralization, it is utilized, often in conjunction with radioisotopes, for bone imaging.

Clodronic acid disodium salt (Lodronate), a bisphosphonate, is a potent antiosteolytic agent which inhibits bone resorption.

Pamidronate Disodium (CGP 23339A), a nitrogen-containing bisphosphonate, can help to strengthen bones.

MBC-11 is a first-in-class conjugate of the bone-targeting bisphosphonate etidronate covalently linked to the antimetabolite cytarabine (araC), with potential to treat tumor-induced bone disease (TIBD).

BPH-1358 (NSC-50460) (NSC-50460) is a potent human farnesyl diphosphate synthase (FPPS) and undecaprenyl diphosphate synthase (UPPS) inhibitor. With IC50s of 1.8 μM and 110 nM, respectively. And it is active against S. aureus in vitro (MIC ~250 ng mL)[1][2].

Ibandronic acid (Bonviva) is a third-generation amino-bisphosphonate with anti-resorptive and anti-hypercalcemic activities.

Ibandronate sodium monohydrate (BM-210955) is a highly potent nitrogen-containing bisphosphonate used for the treatment of osteoporosis.

Cgp 47072 is a bisphosphonate, used in the treatment of bone diseases, particularly where there is uncontrolled bone resorption.

BPH-1358 (NSC50460) free base is a potent human undecaprenyl diphosphate synthase (UPPS) and farnesyl diphosphate synthase (FPPS) inhibitor (IC50s: 110 nM and 1.8 μM) and is active against S. aureus in vitro (MIC ~250 ng mL).

TH-Z93 is a potent FPPS inhibitor (IC50:90 nM) and a lipophilic bisphosphonate.

Tiludronate (Tiludronic Acid) disodium hemihydrate is an orally active bisphosphonate compound used primarily in metabolic bone disorder research. It functions as an osteoregulator and acts as a potent inhibitor of the osteoclast vacuolar H+ -ATPase, possessing antiresorptive and anti-inflammatory properties [4].

MBC-11 trisodium has potential to treat tumor-induced bone disease (TIBD).It is a first-in-class conjugate of the bone-targeting bisphosphonate HEDP covalently linked to the antimetabolite Ara-C.

MBC-11 triethylamine has potential to treat tumor-induced bone disease (TIBD), is a first-in-class conjugate of the bone-targeting bisphosphonate etidronate covalently linked to the antimetabolite cytarabine (araC).

BPH-715 inhibits the liver-stage growth of P. falciparum with an IC50 of 10 μM for P. falciparum exoerythrocytic forms in HepG2 cells.

NE21650, a bisphosphonate, inhibits isopentenyl diphosphate isomerase and farnesyl diphosphate synthase.

HUN47990 is a bisphosphonate (BP) prodrug with antitumor activity. HUN47990 potently inhibits the in vitro growth of a variety of tumor cell lines, especially hematopoietic cell lines, at nanomolar concentrations. HUN47990 inhibited the prenylation of the RAP1A small GTPase signaling protein at concentrations as low as 1-10 nM. HUN47990 slowed the growth of human bladder cancer cells in an immunodeficient mouse model. HUN47990 is significantly more active than zoledronic acid, the most active FDA-approved BP, and a potential anti-cancer therapeutic. HUN47990 was first reported in ChemMedChem. 2016 Dec 16;11(24):2656-2663 (compound 7). This product has no formal name at the moment. For the convenience of communication, a temporary code name was therefore proposed according to MedKoo Chemical Nomenclature (see web page: https://www.medkoo.com/page/naming).

BV600022 is an osteoadsorptive bisphosphonate-ciprofloxacin conjugate with antibacterial activity.

Zoledronic Acid (Zoledronate) disodium tetrahydrate is a potent third-generation bisphosphonate (BP) with strong anti-resorptive activity, effectively inhibiting osteoclast differentiation and apoptosis, and demonstrating anti-cancer properties [1].

Compound 13h (hGGPPS-IN-3) is a potent inhibitor of human geranylgeranyl pyrophosphate synthase (hGGPPS), characterized as a C-2-substituted thienopyrimidine-based bisphosphonate analogue (C2-ThP-BPs). It selectively induces apoptosis in multiple myeloma (MM) cells and demonstrates antimyeloma activity in vivo [1].

Pamidronate monosodium is a bisphosphonate.

Tiludronate (Tiludronic Acid), an orally active bisphosphonate with osteoregulatory activity, is used to study metabolic bone disorders. It acts as a potent inhibitor of osteoclast vacuolar H(+)-ATPase and exhibits antiresorptive and anti-inflammatory properties.

NE 10790 (3-PEHPC) is a phosphonocarboxylate analogue of the potent bisphosphonate risedronate and is a weak anti-resorptive agent. Although NE10790 was a poor inhibitor of FPP synthase