Peringatan Keamanan

The most common toxic effects observed are hyperglycemia, cholelithiasis, diarrhea, nausea, headache, abdominal pain, fatigue, and diabetes mellitus.

Pasireotide

DB06663

small molecule approved

Deskripsi

Pasireotide is a synthetic long-acting cyclic hexapeptide with somatostatin-like activity. It is marketed as a diaspartate salt called Signifor, which is used in the treatment of Cushing's disease.

Struktur Molekul 2D

Berat 1047.2062
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half-life is 12 hours.
Volume Distribusi Pasireotide is widely distributed and has a volume of distribution of >100L.
Klirens (Clearance) The clearance in healthy patient is ~7.6 L/h and in Cushing’s disease patients is ~3.8 L/h.

Absorpsi

The peak plasma concentration of pasireotide occurs in 0.25-0.5 hours. After administration of single and multiple doses, there is dose-proportionoal increases in Cmax and AUC.

Metabolisme

Metabolism is minimal.

Rute Eliminasi

Pasireotide is eliminated mostly by hepatic clearance (biliary excretion)(about 48%) with some minor renal clearance (about 7.63%).

Interaksi Obat

680 Data
Lomitapide The metabolism of Lomitapide can be decreased when combined with Pasireotide.
Bromocriptine The serum concentration of Bromocriptine can be increased when it is combined with Pasireotide.
Ceritinib Pasireotide may increase the bradycardic activities of Ceritinib.
Ivabradine Pasireotide may increase the bradycardic activities of Ivabradine.
Pegvisomant The risk or severity of increased transaminases can be increased when Pasireotide is combined with Pegvisomant.
Ruxolitinib Ruxolitinib may increase the bradycardic activities of Pasireotide.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Pasireotide.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Pasireotide.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Pasireotide.
Colchicine The metabolism of Colchicine can be decreased when combined with Pasireotide.
Fentanyl Fentanyl may increase the bradycardic activities of Pasireotide.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Pasireotide.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Pasireotide.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Pasireotide.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Pasireotide.
Eszopiclone The metabolism of Eszopiclone can be decreased when combined with Pasireotide.
Zopiclone The metabolism of Zopiclone can be decreased when combined with Pasireotide.
Lovastatin The metabolism of Lovastatin can be decreased when combined with Pasireotide.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Pasireotide.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Pasireotide.
Warfarin The serum concentration of Warfarin can be increased when it is combined with Pasireotide.
Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Pasireotide.
(R)-warfarin The serum concentration of (R)-warfarin can be increased when it is combined with Pasireotide.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Pasireotide.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Pasireotide.
(S)-Warfarin The serum concentration of (S)-Warfarin can be increased when it is combined with Pasireotide.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Pasireotide.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Pasireotide.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Pasireotide.
Cyclosporine The bioavailability of Cyclosporine can be decreased when combined with Pasireotide.
Insulin human The risk or severity of hypoglycemia can be increased when Pasireotide is combined with Insulin human.
Insulin lispro The risk or severity of hypoglycemia can be increased when Pasireotide is combined with Insulin lispro.
Insulin glargine The risk or severity of hypoglycemia can be increased when Pasireotide is combined with Insulin glargine.
Insulin pork The risk or severity of hypoglycemia can be increased when Pasireotide is combined with Insulin pork.
Troglitazone The therapeutic efficacy of Troglitazone can be decreased when used in combination with Pasireotide.
Glimepiride The therapeutic efficacy of Glimepiride can be decreased when used in combination with Pasireotide.
Acarbose The therapeutic efficacy of Acarbose can be decreased when used in combination with Pasireotide.
Sulfadiazine The therapeutic efficacy of Sulfadiazine can be decreased when used in combination with Pasireotide.
Rosiglitazone The therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Pasireotide.
Acetohexamide The therapeutic efficacy of Acetohexamide can be decreased when used in combination with Pasireotide.
Miglitol The therapeutic efficacy of Miglitol can be decreased when used in combination with Pasireotide.
Chlorpropamide The therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Pasireotide.
Nateglinide The therapeutic efficacy of Nateglinide can be decreased when used in combination with Pasireotide.
Tolazamide The therapeutic efficacy of Tolazamide can be decreased when used in combination with Pasireotide.
Repaglinide The therapeutic efficacy of Repaglinide can be decreased when used in combination with Pasireotide.
Phenformin The therapeutic efficacy of Phenformin can be decreased when used in combination with Pasireotide.
Sulfamethoxazole The therapeutic efficacy of Sulfamethoxazole can be decreased when used in combination with Pasireotide.
Glyburide The therapeutic efficacy of Glyburide can be decreased when used in combination with Pasireotide.
Glipizide The therapeutic efficacy of Glipizide can be decreased when used in combination with Pasireotide.
Gliclazide The therapeutic efficacy of Gliclazide can be decreased when used in combination with Pasireotide.
Tolbutamide The therapeutic efficacy of Tolbutamide can be decreased when used in combination with Pasireotide.
Pioglitazone The therapeutic efficacy of Pioglitazone can be decreased when used in combination with Pasireotide.
Gliquidone The therapeutic efficacy of Gliquidone can be decreased when used in combination with Pasireotide.
Mitiglinide The therapeutic efficacy of Mitiglinide can be decreased when used in combination with Pasireotide.
Sitagliptin The therapeutic efficacy of Sitagliptin can be decreased when used in combination with Pasireotide.
Exenatide The therapeutic efficacy of Exenatide can be decreased when used in combination with Pasireotide.
Mecasermin The therapeutic efficacy of Mecasermin can be decreased when used in combination with Pasireotide.
Pramlintide The therapeutic efficacy of Pramlintide can be decreased when used in combination with Pasireotide.
Glisoxepide The therapeutic efficacy of Glisoxepide can be decreased when used in combination with Pasireotide.
Insulin aspart The risk or severity of hypoglycemia can be increased when Pasireotide is combined with Insulin aspart.
Insulin detemir The risk or severity of hypoglycemia can be increased when Pasireotide is combined with Insulin detemir.
Insulin glulisine The risk or severity of hypoglycemia can be increased when Pasireotide is combined with Insulin glulisine.
Glymidine The therapeutic efficacy of Glymidine can be decreased when used in combination with Pasireotide.
AICA ribonucleotide The therapeutic efficacy of AICA ribonucleotide can be decreased when used in combination with Pasireotide.
Buformin The therapeutic efficacy of Buformin can be decreased when used in combination with Pasireotide.
Vildagliptin The therapeutic efficacy of Vildagliptin can be decreased when used in combination with Pasireotide.
Voglibose The therapeutic efficacy of Voglibose can be decreased when used in combination with Pasireotide.
NN344 The risk or severity of hypoglycemia can be increased when Pasireotide is combined with NN344.
AMG-222 The therapeutic efficacy of AMG-222 can be decreased when used in combination with Pasireotide.
Bisegliptin The therapeutic efficacy of Bisegliptin can be decreased when used in combination with Pasireotide.
Alogliptin The therapeutic efficacy of Alogliptin can be decreased when used in combination with Pasireotide.
Dapagliflozin The therapeutic efficacy of Dapagliflozin can be decreased when used in combination with Pasireotide.
Saxagliptin The therapeutic efficacy of Saxagliptin can be decreased when used in combination with Pasireotide.
Liraglutide The therapeutic efficacy of Liraglutide can be decreased when used in combination with Pasireotide.
Gosogliptin The therapeutic efficacy of Gosogliptin can be decreased when used in combination with Pasireotide.
Linagliptin The therapeutic efficacy of Linagliptin can be decreased when used in combination with Pasireotide.
Canagliflozin The therapeutic efficacy of Canagliflozin can be decreased when used in combination with Pasireotide.
Glibornuride The therapeutic efficacy of Glibornuride can be decreased when used in combination with Pasireotide.
Benfluorex The therapeutic efficacy of Benfluorex can be decreased when used in combination with Pasireotide.
Empagliflozin The therapeutic efficacy of Empagliflozin can be decreased when used in combination with Pasireotide.
Albiglutide The therapeutic efficacy of Albiglutide can be decreased when used in combination with Pasireotide.
Dulaglutide The therapeutic efficacy of Dulaglutide can be decreased when used in combination with Pasireotide.
Lobeglitazone The therapeutic efficacy of Lobeglitazone can be decreased when used in combination with Pasireotide.
Netoglitazone The therapeutic efficacy of Netoglitazone can be decreased when used in combination with Pasireotide.
Rivoglitazone The therapeutic efficacy of Rivoglitazone can be decreased when used in combination with Pasireotide.
Ciglitazone The therapeutic efficacy of Ciglitazone can be decreased when used in combination with Pasireotide.
Lixisenatide The therapeutic efficacy of Lixisenatide can be decreased when used in combination with Pasireotide.
Insulin beef The risk or severity of hypoglycemia can be increased when Pasireotide is combined with Insulin beef.
Insulin degludec The risk or severity of hypoglycemia can be increased when Pasireotide is combined with Insulin degludec.
Insulin peglispro The risk or severity of hypoglycemia can be increased when Pasireotide is combined with Insulin peglispro.
Insulin tregopil The risk or severity of hypoglycemia can be increased when Pasireotide is combined with Insulin tregopil.
Ipragliflozin The therapeutic efficacy of Ipragliflozin can be decreased when used in combination with Pasireotide.
Dutogliptin The therapeutic efficacy of Dutogliptin can be decreased when used in combination with Pasireotide.
Allicin The therapeutic efficacy of Allicin can be decreased when used in combination with Pasireotide.
Tofogliflozin The therapeutic efficacy of Tofogliflozin can be decreased when used in combination with Pasireotide.
Ertugliflozin The therapeutic efficacy of Ertugliflozin can be decreased when used in combination with Pasireotide.
2,4-thiazolidinedione The therapeutic efficacy of 2,4-thiazolidinedione can be decreased when used in combination with Pasireotide.
Teneligliptin The therapeutic efficacy of Teneligliptin can be decreased when used in combination with Pasireotide.
Omarigliptin The therapeutic efficacy of Omarigliptin can be decreased when used in combination with Pasireotide.
Carmegliptin The therapeutic efficacy of Carmegliptin can be decreased when used in combination with Pasireotide.

Target Protein

Somatostatin receptor type 3 SSTR3
Somatostatin receptor type 1 SSTR1
Somatostatin receptor type 2 SSTR2
Somatostatin receptor type 5 SSTR5

Referensi & Sumber

Synthesis reference: Bruns C, Lewis I, Briner U, Meno-Tetang G, Weckbecker G: SOM230: a novel somatostatin peptidomimetic with broad somatotropin release inhibiting factor (SRIF) receptor binding and a unique antisecretory profile. Eur J Endocrinol. 2002 May;146(5):707-16.
Artikel (PubMed)
  • PMID: 12239124
    Weckbecker G, Briner U, Lewis I, Bruns C: SOM230: a new somatostatin peptidomimetic with potent inhibitory effects on the growth hormone/insulin-like growth factor-I axis in rats, primates, and dogs. Endocrinology. 2002 Oct;143(10):4123-30.

Contoh Produk & Brand

Produk: 43 • International brands: 2
Produk
  • Signifor
    Injection • 0.3 mg/1mL • Subcutaneous • US • Approved
  • Signifor
    Injection • 0.6 mg/1mL • Subcutaneous • US • Approved
  • Signifor
    Injection • 0.9 mg/1mL • Subcutaneous • US • Approved
  • Signifor
    Injection • 0.3 mg/1mL • Subcutaneous • US • Approved
  • Signifor
    Injection • 0.6 mg/1mL • Subcutaneous • US • Approved
  • Signifor
    Injection • 0.9 mg/1mL • Subcutaneous • US • Approved
  • Signifor
    Solution • 0.3 mg / mL • Subcutaneous • Canada • Approved
  • Signifor
    Solution • 0.6 mg / mL • Subcutaneous • Canada • Approved
Menampilkan 8 dari 43 produk.
International Brands
  • Signifor
  • Signifor LAR

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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