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Lasofoxifene | CAS No: 180916-16-9 | GMP-certified suppliers
A medication that reduces fracture risk in postmenopausal osteoporosis and addresses vulvar atrophy and breast cancer risk reduction in postmenopausal women.
Therapeutic categories
Genito Urinary System and Sex HormonesNaphthalenesSelective Estrogen Receptor ModulatorsSex Hormones and Modulators of the Genital System
Generic name
Lasofoxifene
Molecule type
small molecule
CAS number
180916-16-9
DrugBank ID
DB06202
Approval status
Approved drug, Investigational drug
ATC code
G03XC03
Primary indications
- Investigated for use/treatment in postmenopausal osteoporosis to reduce the risk of both vertebral and novertebral fractures, as well as address other postmenopausal conditions, including reduction in risk of breast cancer and treatment of vulvar and vaginal atrophy (VVA)
Product Snapshot
- Lasofoxifene is an oral small molecule formulation available as film-coated tablets
- It is primarily indicated for postmenopausal osteoporosis fracture risk reduction and management of other postmenopausal conditions including breast cancer risk reduction and treatment of vulvar and vaginal atrophy
- Lasofoxifene holds approval in the European Union and is under investigational status in other markets
Clinical Overview
Lasofoxifene (CAS Number 180916-16-9) is a non-steroidal third-generation selective estrogen receptor modulator (SERM) structurally classified as a phenylnaphthalene derivative. It selectively binds with high affinity to both estrogen receptor alpha (ERα) and beta (ERβ) subtypes, exhibiting tissue-specific agonist and antagonist activities.
Clinically, lasofoxifene has been investigated primarily for the prevention and treatment of postmenopausal osteoporosis. It is indicated to reduce the risk of both vertebral and nonvertebral fractures. Additionally, it has been explored for managing vulvar and vaginal atrophy (VVA) and shows potential in lowering the risk of breast cancer among postmenopausal women. The compound mimics the effects of estradiol in bone tissue by reducing osteoclast production and lifespan, modulating the receptor activator of nuclear factor kappa-B ligand (RANKL)/RANK/osteoprotegerin pathway, and stimulating osteoblast activity. It also influences calcium homeostasis favorably.
Lasofoxifene acts as an antagonist in uterine and mammary tissues, suppressing estrogen-driven oncogenic signaling and inhibiting downstream gene transcription relevant to cancer pathways. Notably, preclinical data indicate it may function as an inverse agonist at the CB2 cannabinoid receptor expressed in bone, further contributing to the inhibition of osteoclast formation and activity.
Following its initial development by Pfizer under the brand name Oporia, lasofoxifene was subject to regulatory challenges in the United States but received approval in Europe in 2009 as Fablyn. Ligand Pharmaceuticals holds licensing agreements for development and commercialization, including collaboration with Sermonix Pharmaceuticals for the US market.
Key pharmacokinetic parameters include a favorable oral bioavailability profile typical of SERMs, with distribution to estrogen receptor-rich tissues influencing both efficacy and safety. Safety considerations include typical SERM-associated risks such as thromboembolic events and endometrial effects, necessitating appropriate monitoring in clinical use.
From an API sourcing perspective, lasofoxifene requires high purity consistent with stringent regulatory standards given its therapeutic use. Reliable suppliers will provide comprehensive documentation including certificate of analysis, impurity profiles, and compliance with relevant pharmacopeial or regulatory guidelines to ensure quality and consistency in pharmaceutical manufacturing.
Clinically, lasofoxifene has been investigated primarily for the prevention and treatment of postmenopausal osteoporosis. It is indicated to reduce the risk of both vertebral and nonvertebral fractures. Additionally, it has been explored for managing vulvar and vaginal atrophy (VVA) and shows potential in lowering the risk of breast cancer among postmenopausal women. The compound mimics the effects of estradiol in bone tissue by reducing osteoclast production and lifespan, modulating the receptor activator of nuclear factor kappa-B ligand (RANKL)/RANK/osteoprotegerin pathway, and stimulating osteoblast activity. It also influences calcium homeostasis favorably.
Lasofoxifene acts as an antagonist in uterine and mammary tissues, suppressing estrogen-driven oncogenic signaling and inhibiting downstream gene transcription relevant to cancer pathways. Notably, preclinical data indicate it may function as an inverse agonist at the CB2 cannabinoid receptor expressed in bone, further contributing to the inhibition of osteoclast formation and activity.
Following its initial development by Pfizer under the brand name Oporia, lasofoxifene was subject to regulatory challenges in the United States but received approval in Europe in 2009 as Fablyn. Ligand Pharmaceuticals holds licensing agreements for development and commercialization, including collaboration with Sermonix Pharmaceuticals for the US market.
Key pharmacokinetic parameters include a favorable oral bioavailability profile typical of SERMs, with distribution to estrogen receptor-rich tissues influencing both efficacy and safety. Safety considerations include typical SERM-associated risks such as thromboembolic events and endometrial effects, necessitating appropriate monitoring in clinical use.
From an API sourcing perspective, lasofoxifene requires high purity consistent with stringent regulatory standards given its therapeutic use. Reliable suppliers will provide comprehensive documentation including certificate of analysis, impurity profiles, and compliance with relevant pharmacopeial or regulatory guidelines to ensure quality and consistency in pharmaceutical manufacturing.
Identification & chemistry
| Generic name | Lasofoxifene |
|---|---|
| Molecule type | Small molecule |
| CAS | 180916-16-9 |
| UNII | 337G83N988 |
| DrugBank ID | DB06202 |
Pharmacology
| Summary | Lasofoxifene is a selective estrogen receptor modulator that exerts agonist effects on estrogen receptors in bone, enhancing osteoblast activity and inhibiting osteoclast-mediated bone resorption via modulation of the RANKL/RANK/osteoprotegerin pathway. It functions as an antagonist in uterine and mammary tissues by suppressing estrogen-driven oncogenic signaling. Additionally, lasofoxifene may act as an inverse agonist at the CB2 cannabinoid receptor, further inhibiting osteoclast formation and activity. |
|---|---|
| Mechanism of action | Lasofoxifene mediates an agonist effect on estrogen receptors expressed on bone to mimic the positive effects of estrogen to reduce the production and lifespan of osteoclasts via altering the NF-kappaB ligand (RANKL)/RANK/osteoprotegerin system, stimulation of osteoblast (the bone forming cells) activity and additional effects on calcium homeostasis . It acts as an antagonist at uterus and mammary glands by suppressing the estrogen signaling in oncogenic pathways and inhibits the downstream gene transcription . A study also suggests that lasofoxifene may also act as an inverse agonist at CB2 cannabinoid receptor which is expressed in bone to inhibit osteoclast formation and resorptive activity. |
| Pharmacodynamics | Lasofoxifene exhibits both significant estrogenic and antiestrogenic activity both in vitro and in vivo, targeting any tissues that possess ERs, such as bone, uterus, breast, blood vessels, and liver. Binding assays demonstrated high affinity of the compound for both ERα and ERβ in a tissue-dependent manner. It mimics the effects of estradiol with varying agonist and antagonist effects. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Estrogen receptor alpha | Humans | antagonist, agonist, negative modulator |
| Estrogen receptor beta | Humans | agonist |
| Cannabinoid receptor 2 | Humans | inverse agonist |
ADME / PK
| Absorption | Peak plasma concentrations (Cmax) were reached in about 6.0 to 7.3 hours . Displays higher oral bioavailability compared to other SERMs with increased resistance to intestinal glucuronidation due to nonpolar tetrahydronaphthalene structure . In a comparative study in the rat, lasofoxifene showed bioavailability of 62% . |
|---|---|
| Half-life | Elimination half-life is approximately 6 days . |
| Protein binding | Lasofoxifene is highly bound to plasma proteins (>99%) where it predominantly binds to albumin and α1-acid glycoprotein . |
| Metabolism | Phase I oxidation via hepatic CYP3A4/CYP3A5 and CYP2D6 accounts for nearly half of total metabolism of lasofoxifene. Phase II conjugation reactions include glucuronidation and sulfation. Its glucuronidation is catalyzed by UGTs that are expressed in both the liver (UGT1A1, UGT1A3, UGT1A6, and UGT1A9) and the intestine (UGT1A8 and UGT1A10). Further metabolites of lasofoxifene detected in plasma are the glucuronide of a hydroxylated metabolite, and the methylated catechols . |
| Route of elimination | Primarily fecal excretion and secondarily renal elimination as mainly metabolites, with less than 2% excreted in urine as unchanged parent drug. |
| Volume of distribution | The apparent volume of distribution in postmenopausal women is 1350L . |
| Clearance | The apparent oral clearance (CL/F) of lasofoxifene in postmenopausal women is approximately 6.6 l/hr. |
Formulation & handling
- Lasofoxifene is a small molecule suitable for oral administration, typically formulated as film-coated tablets.
- The compound exhibits low water solubility and high lipophilicity (LogP 5.97), which may require solubilization strategies during formulation.
- No specific sensitivity to food or biologic degradation concerns are noted, facilitating standard oral handling and storage.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient is approaching patent expiry within the EU market, with generic versions expected to enter, indicating a transition toward increased market competition and maturity. |
|---|
| Markets | EU |
|---|
Supply Chain
| Supply chain summary | Lasofoxifene is primarily marketed in the European Union with multiple branded products under the name Fablyn. The presence of several originator companies is implied by the multiple brand entries. Patent expiration status is not specified, so the timing of generic competition cannot be determined from the available data. |
|---|
Safety
| Toxicity | Lasofoxifene increases the risk of venous thromboembolism driven by increased risk of deep vein thrombosis. Other adverse effects include hot flushes, muscle spasms and vaginal bleeding. |
|---|
High Level Warnings:
- Lasofoxifene exposure may increase the risk of venous thromboembolism, including deep vein thrombosis
- Potential adverse effects include musculoskeletal spasms and genitourinary bleeding
- Handling should consider the compound’s prothrombotic properties and systemic vascular impact
Lasofoxifene is a type of Genitourinary Agents
Genitourinary agents are a category of pharmaceutical active ingredients (APIs) that are specifically designed to target and treat disorders related to the genitourinary system. The genitourinary system encompasses the organs and structures involved in the production, storage, and elimination of urine, as well as the reproductive organs.
These APIs play a crucial role in the treatment of various genitourinary conditions, including urinary tract infections (UTIs), erectile dysfunction, urinary incontinence, benign prostatic hyperplasia (BPH), and other related disorders. They exert their therapeutic effects by interacting with specific receptors or enzymes in the genitourinary system, regulating physiological processes, and restoring normal function.
Some commonly used genitourinary agents include alpha-blockers, which relax the smooth muscles in the prostate and bladder neck, improving urine flow in patients with BPH. Additionally, phosphodiesterase type 5 inhibitors (PDE5 inhibitors) are widely prescribed for erectile dysfunction, as they enhance blood flow to the penile tissues, facilitating erection.
These APIs are typically formulated into various dosage forms, such as tablets, capsules, creams, gels, or injections, allowing for convenient administration to patients. The development and production of genitourinary agents involve stringent quality control measures and compliance with regulatory guidelines to ensure safety, efficacy, and consistent product performance.
In summary, genitourinary agents form a crucial category of pharmaceutical APIs used to treat a range of disorders affecting the genitourinary system. Their targeted mechanisms of action and diverse dosage forms make them valuable tools in improving genitourinary health and enhancing patients' quality of life.
