Teriparatide is the N-terminal 1-34 active fragment of recombinant human parathyroid hormone (PTH), belonging to the class of synthetic polypeptide hormones. It is the world's first approved "anabolic agent" that directly stimulates osteoblast activity and promotes new bone formation by mimicking the physiological effects of endogenous PTH, rather than simply inhibiting bone resorption like traditional drugs. Common brand names include Forsteo® and Xinfutai®.
Research Background: Parathyroid extracts were discovered to promote bone growth as early as the 1920s, but it wasn't until the 1970s that scientists like John Parsons restarted research and confirmed the effect of the PTH (1-34) fragment in promoting bone mass increase.
Launch History: First developed by Eli Lilly, it was approved by the US FDA in November 2002, becoming the world's first anabolic agent. The original Chinese-developed product (Fotai®) was approved for import in March 2011, and the first domestically produced product (United Cell) was approved in 2017. Products from companies like Sinopharm subsequently entered the market.
Sequence: H-Ser-Val-Ser-Glu-Ile-Gln-Leu-Met-His-Asn-Leu-Gly-Lys-His-Leu-Asn-Ser-Met-Glu-Arg-Val-Glu-Trp-Leu-Arg-Lys-Lys-Leu-Gln-Asp-Val-His-Asn-Phe-OH (34 amino acids).
Molecular Formula: C₁₈₁H₂₉₁N₅₅O₅₁S₂ (free base), acetate form often includes C₂H₄O₂.
Molecular Weight: Approximately 4117.72 Da (free base), teriparatide acetate approximately 4177.77 Da.
CAS Number: 52232-67-4.
Common Specifications: 20 μg / 80 μL (i.e., 250 μg/mL), usually 2.4 mL/vial (pre-filled syringe pen) or 200 IU / 20 μg/bottle (lyophilized powder).
Storage: Refrigerate at 2–8 °C, protected from light; generally do not freeze.
Recommended Dosage: 20 μg (80 μL) once daily, subcutaneously (usually in the thigh or abdomen).
Treatment Duration Limitations: The maximum total treatment duration is 24 months, and patients can only receive one 24-month treatment course in their lifetime (after which teriparatide should not be used again; other anti-bone resorption drugs can be used instead).
Supportive Supplements: If dietary intake is insufficient, calcium and vitamin D supplementation is necessary.
Pharmacokinetics: After subcutaneous injection of 20 μg, Tmax is approximately 30 minutes, half-life is approximately 1 hour, and absolute bioavailability is approximately 95%.
Pulsatile Bone Formation Promotion: Once-daily intermittent (pulsatile) administration transiently activates PTH1R receptors on the surface of osteoblasts, promoting osteoblast proliferation and differentiation and inhibiting apoptosis, thereby increasing bone formation; this is the opposite of the bone resorption effect of persistently high PTH levels (such as in hyperparathyroidism).
Improved Bone Microstructure: It not only increases bone mineral density (BMD) but also increases trabecular bone thickness and connectivity, improving bone quality and strength.
Clinical Efficacy: After 48 weeks of treatment, lumbar vertebral BMD increases by approximately 5.75% from baseline; it significantly reduces the risk of vertebral fractures by 65%–77%, and also significantly reduces the risk of non-vertebral fractures.
Unique Bone Formation Promoter: For a considerable period, it is the only approved anabolic anti-osteoporosis drug in China, increasing new bone from the "source."
Powerful Bone Mineral Density Enhancement: For high-risk individuals with severe osteoporosis or multiple vertebral fractures, its effect in increasing bone mineral density and reducing fracture risk is often superior to simple anti-resorption drugs (such as bisphosphonates).
Seamless Transition to Subsequent Treatment: After the 24-month treatment course, bisphosphonates and other medications can be seamlessly integrated to maintain efficacy.
Osteosarcoma Risk (Animal/Warning): Long-term, high-dose administration of teriparatide to rats may increase the incidence of osteosarcoma (malignant bone tumors) in a dose-related manner; although rare in human clinical practice, the package insert still includes a boxed warning, limiting lifetime use to no more than 24 months.
Transient Hypercalcemia: Serum calcium may slightly increase 4–6 hours after injection, returning to baseline within 16–24 hours; routine monitoring of serum calcium is usually not required, but related symptoms should be observed.
Common Adverse Reactions: Nausea (approximately 8.77%), limb pain, headache, dizziness, leg cramps, etc., mostly transient.
Inconvenience and Limitations of Administration: Requires daily subcutaneous injection (mostly pen-based), and is relatively expensive; requires refrigeration; contraindicated in severe renal insufficiency, hypercalcemia, etc.
Limited Evidence for Hip Fractures: Evidence for reducing the risk of hip fractures is less sufficient than for vertebral fractures.
Postmenopausal women: Postmenopausal women with osteoporosis at high risk of fracture (e.g., history of vertebral/non-vertebral fractures, extremely low bone mineral density, or failure/intolerance to other treatments).
Men: Men with primary or hypogonadal osteoporosis at high fracture risk (covered by both FDA and Chinese guidelines).
Glucocorticoid-induced osteoporosis: Osteoporosis at high fracture risk caused by long-term systemic hormone therapy (e.g., prednisone ≥5 mg/day) (both men and women).
Clinical positioning: Often recommended for initial or sequential treatment (e.g., promoting bone formation first, then inhibiting bone resorption) in patients with "extremely high fracture risk".
Contraindications: Hypersensitivity to teriparatide or excipients; pregnancy/lactation; hypercalcemia; severe renal insufficiency; metabolic bone diseases other than primary/hormone-induced osteoporosis (e.g., hyperparathyroidism, Paget's disease); unexplained elevation of alkaline phosphatase; bone tumors/metastases; previous bone radiotherapy; children and adolescents with open epiphyses.
Use with Caution: Active urinary tract stones (may worsen); moderate renal insufficiency; hepatic insufficiency (limited data); use of digitalis (high calcium may induce toxicity).
Orthostatic hypotension: Transient orthostatic hypotension may occur during the first few doses (approximately 4 hours after injection). It is recommended to administer the first dose under medical supervision. The patient can lie flat for a short time after administration.
Blood sampling time: If blood calcium monitoring is required, blood should be drawn 16 hours after the last injection (avoiding the transient increase period).
Lifetime Limitation: Each patient can only receive this treatment once in their lifetime, for a maximum of 24 months. It cannot be repeated.
Self-Injection Training: Patients/caregivers must receive professional injection training, use new needles, and not use the treatment if the medication is cloudy or contains particles.
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