Platinum and Palladium Polyamine Complexes as Anticancer Agents: The Structural Factor

Table 1

Platinum anticancer agents with amine ligands.

Compound	CAS no.	^gMOA	Development phase	Toxicity
Cisplatin [17, 18, 21]	15663-27-1	Covalent binding short-range, intrastrand	Clinically approved	Nephrotoxicity
Carboplatin [12, 303]	41575-94-4	Covalent binding short-range, intrastrand	Clinically approved	Myelosuppression reduced nephrotoxicity
Oxaliplatin [105–107]	61825-94-3	Covalent binding short-range, intrastrand	Clinically approved	Neurotoxicity
Satraplatin [113, 114, 355]	129580-63-8	Covalent binding short-range, intrastrand	Phase III clinical trials	Myelosuppression no significant oto-, neuro-, or nephrotoxicity
Picoplatin [114, 122–124]	181630-15-9	Covalent binding short-range, intrastrand	Phase III clinical trials	Neutropenia no neuro- or nephrotoxicity
BBR3464 [185]	172903-00-3	Covalent binding long-range, interstrand	^hPhase II clinical trials	Neutropenia anemia
^aAH44 [186, 216]	—	Non-covalent interaction electrostatic, H-bonding phosphate clamps	—	—
^bTriplatinNC [186–188]	—	Non-covalent interaction electrostatic, H-bonding phosphate clamps	—	—
^cLipoplatin [136]	15663-27-1	Covalent binding short-range, intrastrand controlled drug delivery	Phases II and III clinical trials	Negligible neuro- and nephrotoxicity
^dLipoxal [141, 142]		Covalent binding short-range, intrastrand controlled drug delivery	Phase I clinical trials	Mild neutropenia no reno-, cardio-, or hepatotoxicity
^eAroplatin [144]	114488-24-3	Covalent binding short-range, intrastrand controlled drug delivery	^iPhases I and II clinical trials	Myelosuppression mild nephrotoxicity
^fProlindac [130]	674289-90-8	Covalent binding short-range, intrastrand controlled drug delivery	Phase II clinical trials	Negligible neurotoxicity

^aComprising two (H₂N(CH₂)₆NH₂)₂) groups substituting the leaving chlorides in BBR3464, n = 8+. ^bComprising two NH₃⁺ groups substituting the leaving chlorides in BBR3464, n = 6+. ^cLipoplatin: liposomal formulation of cisplatin; ^dLipoxal: liposomal formulation of oxaliplatin; ^eAroplatin: liposomal formulation of an oxaliplatin analogue. ^fNanopolymer-oxaliplatin conjugate. ^gMOA: mechanism of action. ^hDid not progress to Phase III, due to plasma decomposition and severe toxicity in Phase II human clinical trials. ⁱDevelopment halted due to economic reasons.