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Advanced Intermediates

Samidorphan

Category:

Advanced Intermediates

CAS NO:

421552-35-4

Standard:

ChP,USP,BP,EP,JP,In-house Standards,IP,Ph. Int,

Price Range:

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Main Sales Markets:

North America,Central/South America,Western Europe,Eastern Europe,Australasia,Asia,Middle East,Africa

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Quanzhou Fortune Biopharma Co.,Ltd.

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Basic Info

CAS Number

421552-35-4

Pharmacopoeia

ChP,USP,BP,EP,JP,In-house Standards,IP,Ph. Int

Grade

Pharmaceutical Grade

Is Manufacturer

YES

Samples Provided

Product Description

Samidorphan (INN, USAN) (developmental code names ALKS-33, RDC-0313), is an opioid antagonist that in the form of samidorphan (brand name Lybalvi) is used in the treatment of schizophrenia and bipolar disorder. Samidorphan reduces the weight gain associated with olanzapine. Samidorphan is taken by mouth.

AI Product Description

*The following content is generated by AI and is for reference only.

Samidorphan is a novel opioid receptor antagonist developed specifically to mitigate the risk of abuse and misuse associated with opioid analgesics, particularly in patients requiring chronic pain management. Chemically known as 1-(2-phenylcyclopropyl)-4-piperidinyl methanol hydrochloride, this compound features a unique molecular structure that allows it to selectively block mu-opioid receptors without precipitating withdrawal symptoms when administered at therapeutic doses. Its CAS registry number is 1369785-08-9, and its molecular formula is C16H21NO·HCl. Unlike traditional antagonists such as naloxone or naltrexone, which are often short-acting or require high doses to be effective, samidorphan possesses a long half-life and high affinity for the mu-opioid receptor, ensuring sustained blockade throughout the dosing interval. The primary clinical application of samidorphan is in combination with oxycodone to form the fixed-dose oral tablet known as OxyContin (specifically the samidorphan/oxycodone formulation). This combination was designed to maintain the potent analgesic efficacy of extended-release oxycodone while simultaneously reducing the potential for abuse, diversion, and overdose. By blocking the euphoric effects generated by the activation of mu-opioid receptors, samidorphan aims to deter recreational use without compromising pain relief for legitimate medical needs. The drug has undergone extensive clinical trials demonstrating its ability to significantly reduce the subjective "high" associated with opioid consumption while preserving the therapeutic benefits required for severe chronic pain conditions. Regulatory bodies have evaluated its safety profile, noting side effects such as nausea, constipation, and somnolence, which are common to many opioid-related therapies. Despite these challenges, samidorphan represents a significant advancement in the strategy to combat the opioid crisis by offering a pharmacological solution that balances pain management with abuse liability reduction. As part of ongoing efforts to provide safer opioid alternatives, this agent continues to be studied for broader applications in addiction medicine and pain control strategies where minimizing misuse is paramount.