Orforglipron

Brand Names: Foundayo

Drug Class: General Prescription

Overview

11 DESCRIPTION FOUNDAYO contains orforglipron, a GLP-1 receptor agonist. The molecular formula for orforglipron calcium is C 48 H 47 F 2 N 10 O 5 .[0.5]Ca and the molecular weight is 902.0 g/mol. The chemical name is calcium bis{3-[(1 S ,2 S )-1-({2-(4-fluoro-3,5-dimethylphenyl)-3-({3-[3-(4-fluoro-1-methyl-1 H -indazol-5-yl)-2-oxo-2,3-dihydro-1 H -imidazol-1-yl]-4-methyl-2,4,6,7-tetrahydro-5 H...

Mechanism of Action

12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action FOUNDAYO is a GLP-1 receptor agonist that binds to and activates the human GLP-1 receptor. GLP-1 is a physiological regulator of appetite and caloric intake. GLP-1 receptors are present in brain regions that regulate appetite. In animal studies, orforglipron distributed to and activated neurons in brain regions that regulate appetite and food intake. 12.2 Pharmacodynamics FOUNDAYO reduces body weight, with greater fat mass loss than lean mass loss. FOUNDAYO decreases food intake. This effect is likely mediated by decreased appetite. FOUNDAYO delays gastric emptying. The delay is largest after the first dose and diminishes over time. Cardiac Electrophysiology At 1.

Indications

  • 1 INDICATIONS AND USAGE FOUNDAYO TM is indicated in combination with a reduced-calorie diet and increased physical activity to reduce excess body weight and maintain weight reduction long term in adults with obesity or adults with overweight in the presence of at least one weight-related comorbid condition. FOUNDAYO™ is a GLP-1 receptor agonist indicated in combination with a reduced-calorie diet and increased physical activity to reduce excess body weight and maintain weight reduction long term in adults with obesity or adults with overweight in the presence of at least one weight-related...

Common Doses

  • 0.8 mg
  • 2.5 mg
  • 5.5 mg
  • 9 mg

Dosage

2 DOSAGE AND ADMINISTRATION Take FOUNDAYO orally once daily, with or without food. ( 2.1 ) Swallow tablets whole. Do not break, crush, or chew. ( 2.1 ) Do not take more than one tablet per day. ( 2.1 ) Starting dosage is 0.8 mg once daily. After at least 30 days, increase dosage to 2.5 mg once daily. ( 2.1 ) After at least 30 days on the 2.5 mg dosage, increase dosage to 5.5 mg once daily. ( 2.1 ) Dosage may be increased to the next dosage level (9 mg, 14.5 mg, or 17.2 mg once daily) after at least 30 days on the current dosage, based on treatment response and tolerability. ( 2.

Black Box Warning

WARNING: RISK OF THYROID C-CELL TUMORS In products with glucagon-like peptide-1 (GLP-1) receptor agonist activity that are pharmacologically active in rats and mice, rodent thyroid C-cell tumors (adenomas and carcinomas) have been observed at clinically relevant exposures and are considered GLP-1 receptor-dependent effects in rodents. Orforglipron is not pharmacologically active in rats or mice and did not produce tumors in rodents [see Nonclinical Toxicology ( 13.1 )] .

Contraindications

  • 4 CONTRAINDICATIONS FOUNDAYO is contraindicated in patients with: A personal or family history of MTC or in patients with MEN 2 [see Warnings and Precautions ( 5.1 )] . Known serious hypersensitivity to orforglipron or any of the excipients in FOUNDAYO. Serious hypersensitivity reactions, including anaphylaxis and angioedema, have been reported with GLP-1 receptor agonists [see Warnings and Precautions ( 5.6 ), Adverse Reactions ( 6.2 )] . Personal or family history of MTC or in patients with MEN 2 ( 4 ) Known serious hypersensitivity to orforglipron or any of the excipients in FOUNDAYO ( 4 )

Side Effects

  • 6 ADVERSE REACTIONS The following serious adverse reactions are described below or elsewhere in the prescribing information: Risk of Thyroid C-Cell Tumors [see Warnings and Precautions ( 5.1 )] Acute Pancreatitis [see Warnings and Precautions ( 5.2 )] Severe Gastrointestinal Reactions [see Warnings and Precautions ( 5.3 )] Acute Kidney Injury Due to Volume Depletion [see Warnings and Precautions ( 5.4 )] Hypoglycemia [see Warnings and Precautions ( 5.5 )] Hypersensitivity Reactions [see Warnings and Precautions ( 5.

Interactions

  • 7 DRUG INTERACTIONS Strong CYP3A4 Inhibitors: The maximum dosage of FOUNDAYO is 9 mg once daily when used concomitantly with a strong CYP3A4 inhibitor. Avoid concomitant use with strong CYP3A4 inhibitors that also inhibit OATP1B. ( 7.1 ) CYP3A4 Inducers: Avoid concomitant use with strong CYP3A4 inducers. Monitor FOUNDAYO effectiveness and escalate dosage as needed when used concomitantly with moderate CYP3A4 inducers. ( 7.1 ) Simvastatin: Do not exceed simvastatin 20 mg once daily when used concomitantly with FOUNDAYO. ( 7.