Welcome to “A to Z: Drugs in Highlight
This series is designed to delve into the intricate realm of pharmaceutical drugs. As the world of pharmaceuticals continues to evolve with new discoveries and emerging challenges, we aim to shed light on the diverse array of medications available today, ranging from blockbuster medications to those that may not be as familiar. Whether you’re a healthcare professional, a student, or simply someone with a curious mind, “A to Z: Drugs in Highlight” promises to be an enlightening and engaging series.
R is for REXULTI®
REXULTI® (from Otsuka Pharmaceutical), also sold under the brand name RXULTI®, is an antipsychotic medicine used to treat schizophrenia in adults. It is also used as an adjunctive therapy for the treatment of major depressive disorder.
How it works:
The active substance in REXULTI® is brexpiprazole. Brexpiprazole works by adjusting the balance of neurotransmitters in the brain, particularly dopamine and serotonin. Brexpiprazole acts inter alia as a partial agonist at serotonin 5-HT1A and dopamine D2 receptors and as an antagonist at serotonin 5-HT2A receptors. This modulation helps normalise the activity of the brain and reduce symptoms of depression and schizophrenia.
REXULTI® is available as tablets (0.25, 0.5, 1, 2, 3 and 4 mg) to be taken by mouth.
Market impact:
REXULTI® is approved for marketing in numerous countries including in the United States (approved by the FDA in July 2015) and Europe (approved by the EMA in July 2018).
REXULTI® reportedly generated DKK 4.5 billion (approximately USD 650 million) in 2023. This marked a 20% increase in revenue compared to the previous year, reflecting the growing demand for REXULTI®.
Patent protection:
There are patent rights protecting QUVIVIQ® in the United States and Europe.
In Europe, EP1869025 relates to a heterocyclic compound represented by the formula (1):
The ring Q, A and R2 being broadly defined. Brexpiprazole is specifically protected in claim 7. Interestingly, Otsuka Pharmaceutical filed a request for central limitation under Article 105a EPC at the European Patent Office in 2015 to limit the list of compounds in granted claim 7 to the first compound, which is “7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof” (i.e., limit the list of compounds in granted claim 7 to brexpiprazole).
US7888362B2 provides a similar scope of protection in the United States.
Otsuka Pharmaceutical has been awarded supplementary protection certificates (SPCs) across Europe for “Brexpiprazole or a salt thereof”. See, for example, SPC/GB18/038. These SPCs extend the maximum protection period for brexpiprazole until 11 April 2031.
Secondary patents have been filed by Otsuka Pharmaceutical to protect various aspects of the brexpiprazole technology. For example, EP2767285B2 (as maintained in amended form after EPO opposition-appeal proceedings) relates to a tablet comprising 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof as an active ingredient, an excipient (a), a binder (b), a disintegrant (c) and a lubricant (d),
wherein the excipient (a) is at least one member selected from the group consisting of lactose, corn starch, and microcrystalline cellulose;
the binder (b) is hydroxypropyl cellulose;
the disintegrant (c) is at least one member selected from the group consisting of low-substituted hydroxypropyl cellulose, croscarmellose sodium, and sodium carboxymethyl starch; and
the lubricant (d) is magnesium stearate;
the tablet further comprising a coating layer on the surface thereof,
wherein said coating layer comprises a colorant (e), and the colorant (e) comprises iron oxide.
Patent support from Secerna
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