Table 13.
Antithrombotic drugs categorized according to their risk of DDIs and QTc prolongation when used concomitantly with ribociclib and palbociclib.
| Drug | CYP3A4 Substrate |
CYP3A4 Inhibitor |
CYP3A4 Inducer | Membrane transporter substrate | TdP risk | Comments | |
|---|---|---|---|---|---|---|---|
| Antiplatelet | |||||||
| Acetylsalicylic acid | – | – | – | – | Not Known | Low risk of interaction with palbociclib and ribociclib SAFE OPTIONS |
|
| Clopidogrel1 | Minor | – | – | – | Not Known | ||
| Epoprostenol sodium | – | – | – | – | Not Known | ||
| Eptifibatide | – | – | – | – | Not Known | ||
| Iloprost | – | – | – | – | Not Known | ||
| Tirofiban | – | – | – | – | Not Known | ||
| Triflusal | – | – | – | – | Not Known | ||
| Dipyridamole | – | – | – | – | Not Known | ||
| Abciximab | – | – | – | – | Not Known | ||
| Selexipag | Minor | – | – | OATP1B1, OATP1B3, P-gp, BCRP | Not Known | Caution should be exercised in combination with ribociclib or palbociclib | |
| Ticlopidine | Major | – | – | – | Not Known | High risk of DDIs. Should be avoided the combination with ribociclib or palbociclib | |
| Prasugrel | Major3 | – | – | – | Not Known | ||
| Ticagrelor2 | Major Sensitive /NTI |
weak | – | P-gp | Not Known | ||
| Cilostazol | Major | weak | – | – | Known | ||
| Anticoagulants | |||||||
| Heparin and low molecular weight heparin | – | – | – | – | Not Known | Low risk of interaction with palbociclib and ribociclib SAFE OPTIONS |
|
| Acenocoumarol1 | – | – | – | – | Not Known | ||
| Warfarin2 | Minor | – | – | – | Not Known | ||
| Argatroban | – | – | – | – | Not Known | ||
| Bivalirudin | – | – | – | – | Not Known | ||
| Dabigatran2 | – | – | – | P-gp | Not Known | Caution should be exercised in combination with ribociclib or palbociclib | |
| Edoxaban | Minor | – | – | P-gp | Not Known | ||
| Apixaban | Major | – | – | P-gp, BCRP | Not Known | High risk of DDIs. Should be avoided the combination with ribociclib or palbociclib |
|
| Rivaroxaban | Major4 | – | – | P-gp, BCRP | Not Known | ||
Green: Low risk of interaction with palbociclib and ribociclib, SAFE OPTIONS. Orange: Caution should be exercised. Red: High risk of DDIs. Plasmatic concentrations of the CYP3A4 substrate could be increased (or decreased) when used concomitantly with a CYP3A4 inhibitor (or inducer) moderate or strong. NTI: narrow therapeutic index. TdP,Torsades de pointes; gp-P, P-glycoprotein; OATP1B1/3, organic anion transporter polypeptide; BCRP, breast cancer resistance protein.
Not classified risk QT. According to the source consulted (www.crediblemeds.org), the evidence available at this time did not result in a decision for it to be placed in any of the four QT risk categories.
According to the source consulted (www.crediblemeds.org), the drug is under active review for possible risk of QT prolongation and torsades de pointes.
Prasugrel is a pro-drug which is converted to the active metabolite primarily by CYP3A4 and CYP2B6 and to a lesser extent by CYP2C9 and CYP2C19.
Rivaroxaban is moderate sensitive substrate [98].