Seletracetam API Manufacturers

General Description:

Seletracetam, identified by CAS number 357336-74-4, is a notable compound with significant therapeutic applications. Seletracetam is a pyrrolidone derivative and with a structural similarity to newer generation antiepileptic drug levetiracetam. It binds to the same target as levetiracetam but with higher affinity and has shown potent seizure suppression in models of acquired and genetic epilepsy with high CNS tolerability. It is predicted to have low drug-drug interactions and inhibition or induction of any major human metabolizing enzymes. Seletracetam was in Phase II clinical trials under the supervision of the U.S. Food and Drug Administration (FDA) investigated as treatment of epilepsy and partial epilepsy however its development had been put on hold in July 2007. As of 2010, its production was further halted due to the investigation of a newer antiepileptic agent, brivaracetam.

Indications:

This drug is primarily indicated for: Investigated for use/treatment in epilepsy. Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

Seletracetam undergoes metabolic processing primarily in: It undergoes hydrolysis of the acetamide group to form the carboxylic acid metabolite ucb-101596-1, which is pharmacologically inactive. This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Absorption:

The absorption characteristics of Seletracetam are crucial for its therapeutic efficacy: Seletracetam is rapidly absorbed following oral administration, reaching the Cmax within 1 hour and displaying oral bioavailability of >90%. The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Half-life:

The half-life of Seletracetam is an important consideration for its dosing schedule: Approximately 8 hours in healthy young male subjects. This determines the duration of action and helps in formulating effective dosing regimens.

Protein Binding:

Seletracetam exhibits a strong affinity for binding with plasma proteins: Demonstrates low plasma protein binding (<10%). This property plays a key role in the drug's pharmacokinetics and distribution within the body.

Route of Elimination:

The elimination of Seletracetam from the body primarily occurs through: Primarily eliminated through renal excretion. It is as mainly excreted as unchanged drug (30%) and an acidic metabolite ucb-101596-1 (60%). Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Volume of Distribution:

Seletracetam is distributed throughout the body with a volume of distribution of: The volume of distribution is approximately 0.6 L/kg, which is close to that of total body water. This metric indicates how extensively the drug permeates into body tissues.

Clearance:

The clearance rate of Seletracetam is a critical factor in determining its safe and effective dosage: The total apparent clearance is approximately 0.8mL/min/kg. It reflects the efficiency with which the drug is removed from the systemic circulation.

Pharmacodynamics:

Seletracetam exerts its therapeutic effects through: Seletracetam is an antiepileptic agent that targets the presynaptic mechanisms of epilepsy. It interferes with synaptic vesicle exocytosis and neurotransmitter release by binding to synaptic vesicle protein 2A (SV2A) which is involved in synaptic vesicle docking and fusion. It is also a N-type calcium channel blocker that inhibits the abnormal neuronal discharge by inhibiting the calcium channel function and associated calcium currents. Seletracetam markedly reduces epileptiform markers of both hyper-excitability and hyper-synchronization in an in vitro slice model of epilepsy and potently suppresses seizures in in vivo epilepsy models mimicking both partial and generalized epilepsy . The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Seletracetam functions by: Seletracetam binds to SV2A in a stereospecific and selective manner. SV2A is a membrane glycoprotein present in synaptic vesicles of neurons that plays a role as calcium regulators in neurotransmitter release and modulate synaptic networks. Seletracetam is thought to reduce excessive neuronal activity by modulating SV2A function and restoring the ability of a neuron to regulate its neurotransmitter release. Seizure generation induces a sustained membrane depolarization causing a prolonged firing of voltage-dependent calcium currents sufficient to induce a significant rise in calcium concentration. High voltage-activated calcium currents are inhibited by seletracetam by blocking N-type calcium channels in the pyramidal neurons. The drug reduces the degree of calcium influx and decreases the intraneuronal calcium concentration, blocking the abnormal fluctuations in membrane potential occurring during epileptic discharges. This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Classification:

Seletracetam belongs to the class of organic compounds known as alpha amino acids and derivatives. These are amino acids in which the amino group is attached to the carbon atom immediately adjacent to the carboxylate group (alpha carbon), or a derivative thereof, classified under the direct parent group Alpha amino acids and derivatives. This compound is a part of the Organic compounds, falling under the Organic acids and derivatives superclass, and categorized within the Carboxylic acids and derivatives class, specifically within the Amino acids, peptides, and analogues subclass.

Categories:

Seletracetam is categorized under the following therapeutic classes: Agents causing hyperkalemia, Antiarrhythmic agents, Bradycardia-Causing Agents, Calcium Channel Blockers, Cytochrome P-450 CYP3A Substrates, Cytochrome P-450 CYP3A4 Substrates, Cytochrome P-450 Substrates, Pyrrolidines, Vasodilating Agents. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.