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.

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].

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).

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

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

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.

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

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.

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

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.

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).

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).

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.

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

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

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

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

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

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

Pamidronate monosodium is a 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].

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].

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