Peringatan Keamanan

There is no information regarding the LD50 and overdose of rucaparib.

Rucaparib

DB12332

small molecule approved investigational

Deskripsi

Rucaparib is an anticancer drug and poly (ADP-ribose) polymerase (PARP) inhibitor. PARP is an enzyme that plays an essential role in DNA repair.A18745 Rucaparib is proposed to work in several PARP-dependent and PARP-independent mechanisms of action; however, it causes a unique effect of synthetic lethality. By targeting the genetically-mutated cancer cells that lack a DNA repair mechanism, rucaparib causes cancer cell death and reduces tumour growth.A18745,A31354

Rucaparib was granted FDA Breakthrough Therapy designation in April 2015 A18745 and accelerated approval in December 2016.A249240 The drug was later approved by the European Commission in May 2018.L42185 It is currently used to treat recurrent ovarian and prostate cancer in adults.L42155,L42185

Struktur Molekul 2D

Berat 323.371
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean (coefficient of variation) terminal elimination half-life is 26 (39%) hours.[L42155]
Volume Distribusi The mean (coefficient of variation) apparent volume of distribution is 2300 L (21%).[L42155]
Klirens (Clearance) The mean (coefficient of variation) apparent total clearance at steady state is 44.2 L/h (45%).[L42155]

Absorpsi

Rucaparib exhibits a linear pharmacokinetic profile over the dose range from 240 mg to 840 mg twice daily. The mean (coefficient of variation CV) steady-state rucaparib Cmax is 1940 ng/mL (54%) and AUC0-12h is 16900 h x ng/mL (54%) at the approved recommended dosage. The mean AUC accumulation ratio is 3.5 to 6.2 fold. The median Tmax at the steady state is 1.9 hours, with a range of 0 to 5.98 hours at the approved recommended dosage. The mean absolute bioavailability is 36%, with a range of 30 to 45%.L42155 A high-fat meal increased Cmax and AUC0-24h by 20% and 38%, respectively. The Tmax was delayed by 2.5 hours.L42155

Metabolisme

In vitro, rucaparib is primarily metabolized by CYP2D6 and, to a lesser extent, by CYP1A2 and CYP3A4. In addition to CYP-based oxidation, rucaparib also undergoes N-demethylation, N-methylation, and glucuronidation.L42155 In one study, seven metabolites of rucaparib were identified in plasma, urine, and feces.A249245

Rute Eliminasi

Following a single oral dose of radiolabeled rucaparib, unchanged rucaparib accounted for 64% of the radioactivity. Rucaparib accounted for 45% and 95% of radioactivity in urine and feces, respectively.L42155

Interaksi Makanan

3 Data
  • 1. Exercise caution with grapefruit products. Rucaparib is primarily metabolized through CYP2D6 but is also metabolized by CYP3A4 and CYP1A2. Grapefruit inhibits CYP3A4 metabolism, which may increase rucaparib serum levels.
  • 2. Exercise caution with St. John's Wort. Rucaparib is primarily metabolized through CYP2D6 but is also metabolized by CYP3A4 and CYP1A2. St. John's Wort induces CYP3A4 metabolism, which may reduce rucaparib serum levels.
  • 3. Take with or without food. A high-fat meals increases drug exposure but not to a clinically significant extent.

Interaksi Obat

980 Data
Tizanidine The serum concentration of Tizanidine can be increased when it is combined with Rucaparib.
Afatinib Afatinib may decrease the excretion rate of Rucaparib which could result in a higher serum level.
Bosutinib The metabolism of Bosutinib can be decreased when combined with Rucaparib.
Brentuximab vedotin The metabolism of Brentuximab vedotin can be decreased when combined with Rucaparib.
Ledipasvir Ledipasvir may decrease the excretion rate of Rucaparib which could result in a higher serum level.
Lomitapide The metabolism of Lomitapide can be decreased when combined with Rucaparib.
Pazopanib The metabolism of Pazopanib can be decreased when combined with Rucaparib.
Prucalopride The metabolism of Prucalopride can be decreased when combined with Rucaparib.
Ranolazine The serum concentration of Rucaparib can be increased when it is combined with Ranolazine.
Topotecan Rucaparib may decrease the excretion rate of Topotecan which could result in a higher serum level.
Cilostazol The serum concentration of Cilostazol can be increased when it is combined with Rucaparib.
Deferasirox The serum concentration of Rucaparib can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Rucaparib can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Rucaparib can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Rucaparib can be decreased when it is combined with Teriflunomide.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Rucaparib.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Rucaparib.
Everolimus The metabolism of Everolimus can be decreased when combined with Rucaparib.
Brexpiprazole The metabolism of Brexpiprazole can be decreased when combined with Rucaparib.
Colchicine The metabolism of Colchicine can be decreased when combined with Rucaparib.
Fentanyl The metabolism of Fentanyl can be decreased when combined with Rucaparib.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Rucaparib.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Rucaparib.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Rucaparib.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Rucaparib.
Eszopiclone The metabolism of Eszopiclone can be decreased when combined with Rucaparib.
Zopiclone The metabolism of Zopiclone can be decreased when combined with Rucaparib.
Irinotecan The metabolism of Irinotecan can be decreased when combined with Rucaparib.
Lovastatin The metabolism of Lovastatin can be decreased when combined with Rucaparib.
Zolmitriptan The metabolism of Zolmitriptan can be decreased when combined with Rucaparib.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Rucaparib.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Rucaparib.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Rucaparib.
Famotidine The metabolism of Rucaparib can be decreased when combined with Famotidine.
Saxagliptin The metabolism of Saxagliptin can be decreased when combined with Rucaparib.
Conjugated estrogens Rucaparib may decrease the excretion rate of Conjugated estrogens which could result in a higher serum level.
Hydrocortisone The metabolism of Hydrocortisone can be decreased when combined with Rucaparib.
Ranitidine The metabolism of Rucaparib can be decreased when combined with Ranitidine.
Tenofovir alafenamide The serum concentration of Tenofovir alafenamide can be increased when it is combined with Rucaparib.
Taurocholic acid Taurocholic acid may decrease the excretion rate of Rucaparib which could result in a higher serum level.
Dexamethasone acetate Dexamethasone acetate may decrease the excretion rate of Rucaparib which could result in a higher serum level.
Warfarin The metabolism of Warfarin can be decreased when combined with Rucaparib.
Acenocoumarol The metabolism of Acenocoumarol can be decreased when combined with Rucaparib.
(R)-warfarin The serum concentration of (R)-warfarin can be increased when it is combined with Rucaparib.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Rucaparib.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Rucaparib.
(S)-Warfarin The serum concentration of (S)-Warfarin can be increased when it is combined with Rucaparib.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Rucaparib.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Rucaparib.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Rucaparib.
Mirabegron The serum concentration of Rucaparib can be increased when it is combined with Mirabegron.
Abiraterone The serum concentration of Rucaparib can be increased when it is combined with Abiraterone.
Vincristine The metabolism of Vincristine can be decreased when combined with Rucaparib.
Cyproterone acetate The metabolism of Rucaparib can be increased when combined with Cyproterone acetate.
Doxorubicin The metabolism of Doxorubicin can be decreased when combined with Rucaparib.
Lumacaftor The metabolism of Rucaparib can be increased when combined with Lumacaftor.
Primidone The metabolism of Rucaparib can be increased when combined with Primidone.
Albendazole The metabolism of Rucaparib can be increased when combined with Albendazole.
Rifampin The metabolism of Rucaparib can be increased when combined with Rifampicin.
Moxifloxacin The metabolism of Rucaparib can be decreased when combined with Moxifloxacin.
Alosetron The metabolism of Rucaparib can be decreased when combined with Alosetron.
Gatifloxacin The metabolism of Rucaparib can be decreased when combined with Gatifloxacin.
Simeprevir The metabolism of Rucaparib can be decreased when combined with Simeprevir.
Lobeglitazone The metabolism of Rucaparib can be decreased when combined with Lobeglitazone.
Pazufloxacin The metabolism of Rucaparib can be decreased when combined with Pazufloxacin.
Osilodrostat The metabolism of Rucaparib can be decreased when combined with Osilodrostat.
Codeine The metabolism of Codeine can be decreased when combined with Rucaparib.
Cyclosporine The metabolism of Cyclosporine can be decreased when combined with Rucaparib.
Imipramine The metabolism of Imipramine can be decreased when combined with Rucaparib.
Clonidine The metabolism of Clonidine can be decreased when combined with Rucaparib.
Trimipramine The metabolism of Trimipramine can be decreased when combined with Rucaparib.
Pimozide The metabolism of Pimozide can be decreased when combined with Rucaparib.
Gefitinib The metabolism of Gefitinib can be decreased when combined with Rucaparib.
Progesterone The metabolism of Progesterone can be decreased when combined with Rucaparib.
Erlotinib The metabolism of Erlotinib can be decreased when combined with Rucaparib.
Ponatinib The metabolism of Ponatinib can be decreased when combined with Rucaparib.
Dasabuvir The metabolism of Dasabuvir can be decreased when combined with Rucaparib.
Rolapitant The metabolism of Rucaparib can be decreased when combined with Rolapitant.
Tamoxifen The metabolism of Tamoxifen can be decreased when combined with Rucaparib.
Methadone The metabolism of Methadone can be decreased when combined with Rucaparib.
Quinine The metabolism of Rucaparib can be decreased when combined with Quinine.
Duloxetine The metabolism of Rucaparib can be decreased when combined with Duloxetine.
Chlorpromazine The metabolism of Rucaparib can be decreased when combined with Chlorpromazine.
Doxazosin The metabolism of Doxazosin can be decreased when combined with Rucaparib.
Chloroquine The metabolism of Rucaparib can be decreased when combined with Chloroquine.
Nicardipine The metabolism of Rucaparib can be decreased when combined with Nicardipine.
Azelastine The metabolism of Azelastine can be decreased when combined with Rucaparib.
Selegiline The metabolism of Selegiline can be decreased when combined with Rucaparib.
Promethazine The metabolism of Promethazine can be decreased when combined with Rucaparib.
Primaquine The metabolism of Rucaparib can be decreased when combined with Primaquine.
Nifedipine The metabolism of Nifedipine can be decreased when combined with Rucaparib.
Bepridil The metabolism of Bepridil can be decreased when combined with Rucaparib.
Paliperidone The metabolism of Paliperidone can be decreased when combined with Rucaparib.
Yohimbine The metabolism of Yohimbine can be decreased when combined with Rucaparib.
Tesmilifene The metabolism of Tesmilifene can be decreased when combined with Rucaparib.
Benzyl alcohol The metabolism of Benzyl alcohol can be decreased when combined with Rucaparib.
Asunaprevir The metabolism of Rucaparib can be decreased when combined with Asunaprevir.
Metoprolol The metabolism of Rucaparib can be decreased when combined with Metoprolol.
Clobazam The serum concentration of Rucaparib can be increased when it is combined with Clobazam.
Cimetidine The metabolism of Rucaparib can be decreased when combined with Cimetidine.

Target Protein

Poly [ADP-ribose] polymerase 1 PARP1
Poly [ADP-ribose] polymerase 2 PARP2
Protein mono-ADP-ribosyltransferase PARP3 PARP3

Referensi & Sumber

Artikel (PubMed)
  • PMID: 27087632
    Jenner ZB, Sood AK, Coleman RL: Evaluation of rucaparib and companion diagnostics in the PARP inhibitor landscape for recurrent ovarian cancer therapy. Future Oncol. 2016 Jun;12(12):1439-56. doi: 10.2217/fon-2016-0002. Epub 2016 Apr 18.
  • PMID: 28790837
    Dockery LE, Gunderson CC, Moore KN: Rucaparib: the past, present, and future of a newly approved PARP inhibitor for ovarian cancer. Onco Targets Ther. 2017 Jun 19;10:3029-3037. doi: 10.2147/OTT.S114714. eCollection 2017.
  • PMID: 30358186
    Varol U, Kucukzeybek Y, Alacacioglu A, Somali I, Altun Z, Aktas S, Oktay Tarhan M: BRCA genes: BRCA 1 and BRCA 2. J BUON. 2018 Jul-Aug;23(4):862-866.
  • PMID: 28247266
    Syed YY: Rucaparib: First Global Approval. Drugs. 2017 Apr;77(5):585-592. doi: 10.1007/s40265-017-0716-2.
  • PMID: 31250355
    Liao M, Watkins S, Nash E, Isaacson J, Etter J, Beltman J, Fan R, Shen L, Mutlib A, Kemeny V, Papai Z, van Tilburg P, Xiao JJ: Evaluation of absorption, distribution, metabolism, and excretion of (14)C-rucaparib, a poly(ADP-ribose) polymerase inhibitor, in patients with advanced solid tumors. Invest New Drugs. 2020 Jun;38(3):765-775. doi: 10.1007/s10637-019-00815-2. Epub 2019 Jun 27.

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