Opicapone API CAS 923287-50-7

What is Opicapone ?

Opicapone API is a selective and reversible inhibitor of catechol-O-methyltransferase (COMT). On September 7, 2020, Ono Pharmaceutical announced the launch of Opicapone (BIA 9-1067) 25mg tablets in Japan. It is a novel, once-daily, orally administered selective catechol-O-methyltransferase (COMT) inhibitor, indicated for use in combination with levodopa-carbidopa or levodopa-benserazide hydrochloride.

Opicapone is indicated for patients with Parkinson's disease (PD) as adjunctive therapy to levodopa/carbidopa to improve end-of-dose motor fluctuations (advanced efficacy). These patients often use levodopa to relieve symptoms such as bradykinesia, limb stiffness, and tremors; however, it is rapidly metabolized after entering the body, resulting in a short duration of action and a tendency for fluctuating symptoms, including sudden stiffness and immobility. The core function of CS-1268 is to interfere with the key enzymes that break down levodopa in the body's periphery, slow down its metabolism, prolong the duration of levodopa's effect in the body, and stabilize the fluctuations in the condition.

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How does Opicapone help Levodopa work better?

Opicapone helps Levodopa function better by interfering with catechol-O-methyltransferase (COMT). In Parkinson's disease treatment, even with S-(-)-Carbidopa inhibiting Dopamine decarboxylase, a large amount of Levodopa is still degraded by COMT enzymes in the periphery, resulting in waste. Opicapone API is a potent and long-acting COMT inhibitor that effectively interferes with this metabolic pathway, significantly reducing the peripheral conversion loss of Levodopa and thus improving its bioavailability, allowing more microorganisms to cross the blood-brain barrier and enter the brain. This brings two key clinical benefits: firstly, it significantly prolongs the "on" period of good symptom control after each dose; secondly, it shortens the "off" period when the product's effect diminishes and symptoms recur. Clinical data show that taking 50mg (100g, 500g, or 1kg) daily at bedtime can reduce the "off" period by an average of approximately 100-120 minutes and correspondingly prolong the "on" period. In short, Opicapone (BIA 9-1067) essentially shuts down the second "metabolic barrier" of Levodopa in the periphery, allowing the product to reach the brain more fully and for a longer period to exert its effects. However, it should be noted that because it enhances the effects of Levodopa, the dosage of levodopa should often be appropriately reduced under the guidance of a doctor after starting to take it, in order to prevent inducing or aggravating motor disorders.

 

Why does opicapone help with motor fluctuations?

The fundamental reason why Opicapone can alleviate motor fluctuations is that it solves a particularly troublesome problem in Parkinson's disease treatment-the fluctuating blood concentration of levodopa.

In the later stages of Parkinson's disease, the neuronal endings in the brain that buffer dopamine have significantly degenerated. At this point, relying solely on levodopa results in a rollercoaster-like spike and rapid drop in blood concentration upon entering the bloodstream, with a half-life of only about one and a half hours. This "pulsating" stimulation disrupts the brain's motor control network, resulting in a situation where it works, symptoms disappear-the so-called "on" phase; and then, once the effect wears off, the tremors and stiffness return-the "off" phase. This back-and-forth switching is what we call motor fluctuations.

Opicapone (BIA 9-1067) is specifically designed to solve this problem. It effectively inhibits peripheral COMT enzymes, significantly slowing down the metabolism of Levodopa and maintaining a stable effective concentration without fluctuations, thus avoiding drastic "on-off" switching.

The benefits of this mechanism are direct: after each dose, the "on" period (when symptoms are well controlled) becomes longer, while the "off" period (when the effect wears off and symptoms recur) becomes shorter. Clinical data shows that taking 50mg of CS-1268 before bedtime daily can reduce the "off" period by an average of 100-120 minutes, and the "on" period is also prolonged.

To illustrate, without CS-1268, Levodopa is like water poured into a leaky bucket; the water level fluctuates wildly and is unstable. Taking Opicapone API is like plugging the leak in the bucket, allowing the water level to remain stable for a long time. Therefore, CS-1268 does not directly produce dopamine, but rather performs a "pharmacokinetic optimization" on Levodopa-transforming it from a "short-acting, fluctuating" product to a "long-acting, stable" product, thus stabilizing its kinetic fluctuations.

MF of Opicapone

Density	1.80±0.1 g/cm3(Predicted)
InChIKey	ASOADIZOVZTJSR-UHFFFAOYSA-N
Boiling Point	701.1±70.0 °C(Predicted)
Molecular Weight	413.17
Molecular Formula	C15H10Cl2N4O6
Acidity Coefficient (pKa)	4.67±0.38(Predicted)

Specification

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FAQ:

Q1: What should I avoid while taking Opicapone?
It should be avoided when used with non-selective monoamine oxidase inhibitors (such as phenelzine), and patients with pheochromocytoma should not take it; fasting is required for 1 hour before and after taking it; it may cause sudden sleep, so avoid driving or operating machinery; do not stop taking it suddenly; at the same time, be alert for impulse control disorders and orthostatic hypotension.
Q2: Can I drink alcohol while taking CS-1268?
It is not recommended to drink alcohol while taking Opicapone. Alcohol may worsen mood disorders and impulsive behavior, interfere with the body's regulatory functions, and exacerbate discomfort such as dizziness, drowsiness, and sudden daytime fatigue caused by the product. It also increases the risk of orthostatic hypotension, making it easier to feel dizzy and weak when standing up, and increasing the probability of falls. Therefore, for safety and to maintain a stable condition, it is best to abstain from alcohol throughout the entire course of treatment.
Q3: What to do if you forget to take an Opicapone?

Simply skip the missed dose and take it at the same time the next day at the usual dosage. Do not increase the dosage without consulting a doctor to avoid large fluctuations in body concentration, which may cause discomfort and unstable performance. Do not suddenly stop using it on your own either; just maintain a regular schedule and take it on time.  

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