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Details

Stereochemistry ABSOLUTE
Molecular Formula C40H33F3N4O3
Molecular Weight 674.7102
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of DIRLOTAPIDE

SMILES

CN(CC1=CC=CC=C1)C(=O)[C@@H](NC(=O)C2=CC3=C(C=CC(NC(=O)C4=C(C=CC=C4)C5=CC=C(C=C5)C(F)(F)F)=C3)N2C)C6=CC=CC=C6

InChI

InChIKey=TUOSYWCFRFNJBS-BHVANESWSA-N
InChI=1S/C40H33F3N4O3/c1-46(25-26-11-5-3-6-12-26)39(50)36(28-13-7-4-8-14-28)45-38(49)35-24-29-23-31(21-22-34(29)47(35)2)44-37(48)33-16-10-9-15-32(33)27-17-19-30(20-18-27)40(41,42)43/h3-24,36H,25H2,1-2H3,(H,44,48)(H,45,49)/t36-/m0/s1

HIDE SMILES / InChI

Description

Dirlotapide is indicated for the management of obesity in dogs. Dirlotapide is a microsomal triglyceride transfer protein (MTP) inhibitor. It mainly acts locally in the gut to reduce appetite, increase fecal fat and produce weight loss in dogs. The adverse reactions associated with treatment with Dirlotapide include vomiting, loose stools/diarrhea, lethargy, and anorexia.

CNS Activity

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
1.5 nM [IC50]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
SLENTROL

PubMed

Sample Use Guides

In Vivo Use Guide
The initial dosage of SLENTROL is 0.01 mL/kg (0.0045 mL/lb) body weight, administered once daily, for the first 14 days. After the first 14 days of treatment, the dose volume of SLENTROL should be doubled to 0.02 mL/kg (0.009 mL/lb) of body weight, administered once daily for the next 14 days (days 15 to 28 of treatment). Dogs should be weighed monthly and the dose volume adjusted every month, as necessary, to maintain a target percent weight loss of ≥0.7% per week.
Route of Administration: Oral
In Vitro Use Guide
In a murine model investigating intestinal triglyceride transfer protein (MTP) inhibition, dirlotapide demonstrated potent inhibition of intestinal fat absorption with an ED25 of 0.16 mg/kg. In contrast, it was a poor inhibitor of hepatic MTP as demonstrated in a murine model of triglyceride lowering, where it had an ED25 of 6 mg/kg.