ChemicalBook CAS DataBase List 180916-16-9

180916-16-9

Name	Lasofoxifene
CAS	180916-16-9
Molecular Formula	C28H31NO2
MDL Number	MFCD09475650
Molecular Weight	413.55
MOL File	180916-16-9.mol

Chemical Properties

Melting point	110-113°C
Boiling point	572.4±50.0 °C(Predicted)
density	1.150±0.06 g/cm3(Predicted)
storage temp.	Refrigerator
solubility	Chloroform (Slightly), Methanol (Slightly)
form	Solid
pka	10.31±0.60(Predicted)
color	White to Off-White

Hazard Information

Chemical Properties

Off-White Solid

Uses

A next-generation selective estrogen receptor modulator for treating disorders associated with increased bone turnover and osteopenia.

Definition

ChEBI: Lasofoxifene is a member of the class of tetralins that is 5,6,7,8-tetrahydronaphthalen-2-ol in which the hydrogens at positions 5 and 6 are replaced by 4-[2-(pyrrolidin-1-yl)ethoxy]phenyl and phenyl groups, respectively (the 5R,6S-stereoisomer). It is a selective estrogen receptor modulator indicated for the prevention and treatment of osteoporosis in post-menopausal women. It has a role as an antineoplastic agent, a cardioprotective agent, an estrogen receptor agonist, an estrogen receptor antagonist and a bone density conservation agent. It is a member of tetralins, an aromatic ether, a member of naphthols and a N-alkylpyrrolidine.

Clinical Use

Lasofoxifene is a very potent second-generation SERM currently in phase III clinical trials for the treatment and prevention of osteoporosis in postmenopausal women.

in vivo

Lasofoxifene (4 mg/mice; s.c.; 5 day/week; for 43 d) decreases arthritis severity, by reducing cartilage oligomeric matrix protein (COMP), the serum marker of cartilage destruction and reducing serum IL-6 (inflammatory cytokine) levels in mice^[1].
Lasofoxifene (4 mg/mice; s.c.; 5 day/week; for 43 d) protects against generalised bone loss in CIA by increasing trabecular bone mineral density (BMD), cortical thickness in mice^[1].
Lasofoxifene (5, and 10 mg/kg; s.c.; 5 day/week; for 70 d) exerts function of inhibiting primary tumor growth and reducing metastases to the lung and the liver in mice^[3].

Animal Model:	Post-menopausal RA model on OVX (ovariectomised) DBA/1 mice (female DBA/1 mice, 8-10 weeks old, CIA-treated)^[1]
Dosage:	4 mg/mouse/day
Administration:	Subcutaneous injection; 5 days a week from the first signs of arthritis (day 18); 43 days
Result:	Reduced in arthritis severity, including synovial inflammation and destruction of joints reduction. The mean arthritis frequency was 47% while the vehicle group was 81% at 42 days post immunization.

Animal Model:	NSG mices with xenograft tumors model (MIND, mammary intraductal): WT, Y537S and D538G ERα render tumors^[3]
Dosage:	1, 5, or 10 mg/kg
Administration:	Subcutaneous injection; 5 days per week; for 70 days
Result:	Elicited a superior inhibitory effect at a dose of 10 mg/kg, resulted potential tumor shrinkage in Y537S and D538G tumors. And also reduced tumor weight to 60% for Y537S and 50% for D538G at 5 and 10 mg/kg, respectively.

Spectrum Detail

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