Compositions and methods for administering paltusotine to patients with hepatic impairment
Inventors
GOULET, Lance • Humphreys, William • Madan, Ajay • LUO, SHA
Assignees
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Publication Number
US-12208092-B2
Publication Date
2025-01-28
Expiration Date
Abstract
Provided are compositions and methods for administering paltusotine, or a pharmaceutically acceptable salt thereof, to a patient having hepatic impairment.
Core Innovation
The described invention uses paltusotine, an oral SST2 agonist, for treating patients with hepatic impairment. The approach administers a therapeutically effective amount of paltusotine, or a pharmaceutically acceptable salt thereof, to a hepatic-impaired patient as the same amount that would be administered to a patient without hepatic impairment.
The hepatic impairment is characterized using Child-Pugh Score groups, including mild hepatic impairment (5–6), moderate hepatic impairment (7–9), and severe hepatic impairment (10–15). The document also describes oral administration and tablet dosage forms, together with salt and physical form options for paltusotine, including hydrochloride salts and amorphous forms.
The invention is supported by a rationale that paltusotine activates SST2 and shows selectivity/bias for reduced desensitization risk. The document further reports in vivo efficacy in rat/dog and pharmacokinetic and safety results from a Phase 1 single-dose PK/safety study in subjects with mild, moderate, and severe hepatic impairment, and concludes that no clinically meaningful exposure changes were observed and that no dose adjustment is warranted.
Claims Coverage
The partial content identifies two independent claims. Both focus on administering paltusotine to hepatic-impaired patients without dose adjustment, with treatment indications limited to acromegaly, carcinoid syndrome, and/or neuroendocrine tumor.
Same therapeutically effective amount without dose adjustment for hepatic impairment
Administering a therapeutically effective amount of paltusotine, or a pharmaceutically acceptable salt thereof, to a patient with hepatic impairment, where the therapeutically effective amount is the same amount that would be administered to a patient who does not have hepatic impairment, wherein paltusotine is administered to treat acromegaly, carcinoid syndrome and/or neuroendocrine tumor.
Determining hepatic impairment and administering same amount without dose adjustment
Administering to a patient a therapeutically effective amount of paltusotine, or a pharmaceutically acceptable salt thereof, subsequently determining that the patient has hepatic impairment, and administering the same therapeutically effective amount of paltusotine, or a pharmaceutically acceptable salt thereof, to the patient without dose adjustment, wherein paltusotine is administered to treat acromegaly, carcinoid syndrome and/or neuroendocrine tumor.
Across the identified independent claims, the core claim coverage is that hepatic-impaired patients are treated with paltusotine, or a pharmaceutically acceptable salt, using the same therapeutically effective amount as patients without hepatic impairment, including an embodiment where hepatic impairment is determined before administering without dose adjustment. The treatment indications are limited to acromegaly, carcinoid syndrome, and/or neuroendocrine tumor.
Stated Advantages
No dose adjustment is warranted for patients with hepatic impairment, based on similar pharmacokinetic exposure across Child-Pugh groups.
The therapeutically effective amount provided to hepatic-impaired patients is maintained as the same amount that would be administered to patients without hepatic impairment.
Documented Applications
Treatment of acromegaly in patients with hepatic impairment using paltusotine, or a pharmaceutically acceptable salt, administered without dose adjustment.
Treatment of carcinoid syndrome and/or neuroendocrine tumor in patients with hepatic impairment using paltusotine, or a pharmaceutically acceptable salt, administered without dose adjustment.
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