Zoledronic acid

MUSCULO-SKELETAL SYSTEM

Key facts

Zoledronic acid is an ofp drug catalogued in DrugCentral. It was first approved by the EMA in 2001. DrugCentral lists 16 molecular targets, including FDPS, FPPS and Farnesyl pyrophosphate synthase. Recorded indications include Bone Metastases of Solid Tumors, Glucocorticoid Induced Osteoporosis, Humoral hypercalcemia of malignancy and Hypogonadal Osteoporosis in Males.

• Approval status: ofp (first approved 2001 by the EMA).
• Molecular targets: FDPS, FPPS, Farnesyl pyrophosphate synthase and CA2 (16 listed in DrugCentral).
• Indications: Bone Metastases of Solid Tumors, Glucocorticoid Induced Osteoporosis, Humoral hypercalcemia of malignancy, Hypogonadal Osteoporosis in Males and Osteitis deformans and others.
• ATC code: M05BA08 (Bisphosphonates).
• Molecular formula: C5H10N2O7P2; molecular weight 272.09 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (9)

• Bone Metastases of Solid Tumors
• Glucocorticoid Induced Osteoporosis
• Humoral hypercalcemia of malignancy
• Hypogonadal Osteoporosis in Males
• Osteitis deformans
• Osteolytic Lesions of Multiple Myeloma
• Osteoporosis
• Postmenopausal osteoporosis
• Prevention of Glucocorticoid-Induced Osteoporosis

Off-label uses (1)

• Drug-induced osteoporosis

Contraindications (31)

• Acute nephropathy
• Anuria
• Aseptic necrosis of bone of jaw
• Bone pain
• Breastfeeding (mother)
• Chronic heart failure
• Dehydration
• Fracture of femur
• Fragile capillaries
• Hyperkalemia
• Hypernatremia
• Hypocalcemia
• Hypomagnesemia
• Hyponatremia
• Hypoparathyroidism
• Hypophosphatemia
• Hypovolemia
• Impaired renal function disorder
• Intracranial hemorrhage
• Invasive Dental Procedure
• Joint pain
• Malabsorption States
• Muscle pain
• Oliguria
• Pregnancy, function
• Pulmonary congestion
• Severe dehydration
• Severe renal impairment
• Small intestine excision
• Thyroid Surgery
• + 1 more

Mechanism & targets

Molecular targets (16)

Target	Gene	Action	Activity
Farnesyl pyrophosphate synthase	FDPS	inhibitor	Ki 10.15
Farnesyl pyrophosphate synthase, EC 2.5.1.1, EC 2.5.1.10	FPPS	unknown	Ki 8.00
Farnesyl pyrophosphate synthase	—	unknown	Ki 7.96
Carbonic anhydrase 2	CA2	unknown	IC50 7.21
Carbonic anhydrase 14	CA14	unknown	IC50 7.04
Geranylgeranyl pyrophosphate synthase	BTS1	unknown	Ki 6.59
Carbonic anhydrase 12	CA12	unknown	IC50 6.50
Butyrophilin subfamily 3 member A1	BTN3A1	unknown	EC50 6.31
Farnesyl pyrophosphate synthase	Fdps	inhibitor	IC50 6.30
Farnesyl diphosphate synthase	ispA	unknown	IC50 5.96
Geranylgeranyl pyrophosphate synthase	GGPS1	unknown	Ki 5.57
Carbonic anhydrase 9	CA9	unknown	IC50 5.27
72 kDa type IV collagenase	MMP2	unknown	IC50 5.15
Matrix metalloproteinase-14	MMP14	unknown	IC50 4.90
Neutrophil collagenase	MMP8	unknown	IC50 4.75
Matrix metalloproteinase-9	MMP9	unknown	IC50 4.28

Regulatory approvals (2)

Date	Agency	Marketed as	Applicant	Orphan
2001-08-20	FDA	—	NOVARTIS	Yes
2001-03-20	EMA	—	—

ATC classification

ATC code	Therapeutic hierarchy
M05BA08	MUSCULO-SKELETAL SYSTEM › DRUGS FOR TREATMENT OF BONE DISEASES › DRUGS AFFECTING BONE STRUCTURE AND MINERALIZATION › Bisphosphonates
M05BB08	MUSCULO-SKELETAL SYSTEM › DRUGS FOR TREATMENT OF BONE DISEASES › DRUGS AFFECTING BONE STRUCTURE AND MINERALIZATION › Bisphosphonates, combinations

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Osteonecrosis of jaw	18532.0
Exposed bone in jaw	2800.1
Osteonecrosis	2253.3
Bone pain	1660.1
Metastases to bone	1531.2
Malignant neoplasm progression	1155.9
Pain in jaw	1045.3
Atypical femur fracture	861.7
Bone disorder	861.0
Neutropenia	805.5
Influenza like illness	797.6
Myalgia	797.0

Chemical structure

• Molecular formula: C₅H₁₀N₂O₇P₂
• Molecular weight: 272.09 g/mol
• CAS number: 118072-93-8
• InChIKey: XRASPMIURGNCCH-UHFFFAOYSA-N
• PubChem CID: 68740

OC(CN1C=CN=C1)(P(O)(O)=O)P(O)(O)=O

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Zoledronic acid used for?

DrugCentral lists the following indications for Zoledronic acid: Bone Metastases of Solid Tumors, Glucocorticoid Induced Osteoporosis, Humoral hypercalcemia of malignancy, Hypogonadal Osteoporosis in Males, Osteitis deformans, Osteolytic Lesions of Multiple Myeloma, Osteoporosis and Postmenopausal osteoporosis and others.

How does Zoledronic acid work?

Its molecular targets in DrugCentral include FDPS (inhibitor), FPPS, Farnesyl pyrophosphate synthase and CA2.

When was Zoledronic acid first approved?

Zoledronic acid was first approved by the EMA in 2001.

What is the chemical formula of Zoledronic acid?

Zoledronic acid has the molecular formula C5H10N2O7P2 and a molecular weight of 272.09 g/mol.

Sources

• DrugCentral drug card 2868 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL4303669 — compound record and bioactivity
• PubChem CID 68740 — chemical identifiers
• DrugBank DB00399 — drug record
• FDA UNII 6XC1PAD3KF — substance identity
• DailyMed: FDA labels for Zoledronic acid — current prescribing information (label search)
• UniProt P14324 (FDPS) — target protein
• UniProt P00918 (CA2) — target protein
• UniProt Q9ULX7 (CA14) — target protein
• UniProt O43570 (CA12) — target protein
• UniProt O00481 (BTN3A1) — target protein
• UniProt O95749 (GGPS1) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

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