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Rilzabrutinib (PRN1008) is a reversible covalent, selective, and orally active inhibitor of Bruton‘s tyrosine kinase (BTK). Structurally, Rilzabrutinib features a pyrazolo[3,4‑d]pyrimidine core with a 2‑fluoro‑4‑phenoxyphenyl substituent, a piperidine ring bearing an α,β‑unsaturated nitrile warhead, and a piperazinyl‑oxetanyl side chain.

Ibrutinib (PCI‑32765) is a first‑in‑class, orally bioavailable, irreversible small‑molecule inhibitor of Bruton‘s tyrosine kinase (BTK). Structurally, Ibrutinib features a pyrazolo[3,4‑d]pyrimidine core with a 4‑phenoxyphenyl substituent at the 3‑position, an aminopyrimidine moiety, and a piperidine ring bearing an acrylamide Michael acceptor. This molecular architecture enables Ibrutinib to form a covalent bond with Cys481 in the ATP‑binding pocket of BTK through the acrylamide warhead, resulting in irreversible enzyme inhibition.

Fenebrutinib (GDC‑0853, RG7845) is a potent, selective, orally available, and non‑covalent Bruton‘s tyrosine kinase (BTK) inhibitor developed by Roche/Genentech. Structurally, Fenebrutinib features a complex fused heterocyclic core with a hydroxymethyl‑substituted bipyridinyl scaffold, a piperazinyl‑oxetanyl substituent, and a cyclopenta‑pyrrolo‑pyrazinone moiety.

Bepotastine is a second‑generation, non‑sedating, selective histamine H1 receptor antagonist belonging to the piperidine chemical class. Structurally, Bepotastine features a piperidine ring substituted with a (4‑chlorophenyl)(pyridin‑2‑yl)methoxy group at the 4‑position and a butanoic acid side chain at the 1‑position, with a single stereocenter at the benzylic carbon.

Venetoclax (ABT-199, GDC-0199) is a first-in-class, orally bioavailable small-molecule inhibitor of the B‑cell lymphoma 2 (BCL‑2) protein. Structurally, Venetoclax features a complex heterocyclic core anchored by a biaryl acylsulfonamide pharmacophore, with a nitro‑substituted benzenesulfonamide moiety and a tetrahydropyran-containing substituent that together confer exquisite selectivity for BCL‑2 over other anti‑apoptotic BCL‑2 family members.

Abemaciclib (CAS 1231929-97-7, LY2835219, Verzenio®) is a reversible, ATP-competitive inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6). Structurally, Abemaciclib features a 2-aminopyrimidine core substituted with a fluorinated benzimidazole moiety and an N-ethylpiperazinylmethyl pyridine side chain. The molecule contains two fluorine atoms, eight nitrogen atoms, and a molecular framework that enables potent and selective inhibition of CDK4/cyclin D1 over CDK6/cyclin D1 complexes.