Table 4.
A comparison of drug-combination nanoparticle products CPX-351 and TLC-ART 101 with respect to physical and pharmacokinetic characteristics and manufacturing process.
CPX-351a | TLC-ART 101b | |
---|---|---|
Disease indication | Acute myeloid leukaemia | HIV/AIDS |
Physical properties | ||
Characteristics | liposomes | Drug combination particles (excipient stabilised drug particles) |
Hydrodynamic size | 100 ± 20 nm | ~52 nm |
Excipients | DSPC, DSPG, cholesterol | DSPC, DSPE-mPEG2000 |
Drugs and solubility | Daunorubicin (LogP = 1.83); Cytarabine (LogP = −2.8) | Lopinavir (LogP = 5.94); Ritonavir (LogP = 4.24); Tenofovir (LogP = −1.6) |
Drug ratios (molar)c | 1:5 | 4:1:5 |
Manufacturing process | ||
Manufacturing stepsd |
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Pharmacokinetic characteristics | ||
t1/2 | 31.5 h (Daunorubicin), 40.4 h (Cytarabine) | 476.9 h (Lopinavir), 44.1 h (Ritonavir), 65.3 h (Tenofovir) |
CPX-351 is a liposomal formulation consisting daunorubicin and cytarabine with fixed ratio for treatment of AML.
TLC-ART 101 is a lipid nanoparticle formulation consisting lopinavir, ritonavir and tenofovir with fixed ratio for treatment of HIV/AIDS.
Drug ratios in these formulations molar ratios of daunorubicin:cytarabine and lopinavir:ritonavir:tenoforvir, respectively.
The steps indicate simplified key procedures in manufacturing of CPX-351 and TLC-ART 101.