LASOFOXIFENE HCL Property

Melting point:

185 °C(dec.)

storage temp. 

2-8°C

solubility 

DMSO: soluble10mg/mL, clear

form 

powder

color 

white to beige

Safety

WGK Germany 

3

HS Code 

2933.99.7500

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

LASOFOXIFENE HCL Chemical Properties,Usage,Production

Uses

disintegrant, enteric coating, sustained release formulations

Biological Activity

lasofoxifene (tartrate) is a third-generation, nonsteroidal selective estrogen receptor modulator (serm).estrogen receptors are activated by the hormone estrogen (17β-estradiol). serms are characterized by having estrogen agonist action in some tissues while acting as estrogen antagonists in others [1][2].lasofoxifene, also known as cp 336,156, is a third-generation, nonsteroidal selective estrogen receptor modulator. lasofoxifene bound with high affinity to the human estrogen receptor-α with ic50 value of 1.5 nm [1]. lasofoxifene is also a cb2 inverse agonist [4].in aged female rats, lasofoxifene decreased total serum cholesterol and fat body mass, and no uterine hypertrophy was observed. in 5-month-old ovariectomized (ovx) sprague-dawley female rats, lasofoxifene completely prevented ovx-induced increases in body weight gain, total serum cholesterol, and serum osteocalcin. cp-336,156 completely prevented ovx-induced bone loss and inhibited the increased bone turnover associated with estrogen deficiency in lumbar vertebrae, proximal tibiae, and distal femora [1].in postmenopausal women with osteoporosis, lasofoxifene reduced risks of nonvertebral and vertebral fractures, er-positive breast cancer, coronary heart disease, and stroke but an increased risk of venous thromboembolic events [2][3].

Biochem/physiol Actions

Lasofoxifene is a third-generation selective estrogen receptor modulator (SERM).

References

[1]. ke hz, paralkar vm, grasser wa, et al. effects of cp-336,156, a new, nonsteroidal estrogen agonist/antagonist, on bone, serum cholesterol, uterus and body composition in rat models. endocrinology. 1998 apr;139(4):2068-76.
[2]. cummings sr, ensrud k, delmas pd, et al. lasofoxifene in postmenopausal women with osteoporosis. n engl j med. 2010 feb 25;362(8):686-96.
[3]. gennari l, merlotti d, nuti r. selective estrogen receptor modulator (serm) for the treatment of osteoporosis in postmenopausal women: focus on lasofoxifene. clin interv aging. 2010 feb 2;5:19-29.
[4]. kumar p, song zh. cb2 cannabinoid receptor is a novel target for third-generation selective estrogen receptor modulators bazedoxifene and lasofoxifene. biochem biophys res commun. 2014 jan 3;443(1):144-9.