Cytochrome P-450 CYP3A4 Inhibitors (weak)
| Drug | Drug Name | Drug Indication |
|---|---|---|
| DB01254 | Dasatinib | For the treatment of adults with chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia with resistance or intolerance to prior therapy. Also indicated for the treatment of adults with Philadelphia chromosome-positive acute lymphoblastic leukemia with resistance or intolerance to prior therapy. |
| DB01259 | Lapatinib | Indicated in combination with capecitabine for the treatment of patients with advanced or metastatic breast cancer whose tumors overexpress the human epidermal receptor type 2 (HER2) protein and who have received prior therapy including an anthracycline, a taxane, and trastuzuma. |
| DB00908 | Quinidine | For the treatment of ventricular pre-excitation and cardiac dysrhythmias |
| DB06589 | Pazopanib | Treatment of advanced renal cell cancer and advanced soft tissue sarcoma (in patients previously treated with chemotherapy) |
| DB00818 | Propofol | Used for induction and/or maintenance of anaesthesia and for management of refractory status epilepticus. |
| DB08820 | Ivacaftor | When used as monotherapy as the product Kalydeco, ivacaftor is indicated for the managmenet of CF in patients age 2 years and older who have a mutation in the CFTR gene that is responsive to ivacaftor potentiation. Ivacaftor received expanded approval in May 2017 for the following 33 CFTR mutations: E56K, P67L, R74W, D110E, D110H, R117C, R117H, G178R, E193K, L206W, R347H, R352Q, A455E, S549N, S549R, G551D, G551S, D579G, S945L, S977F, F1052V, K1060T, A1067T, G1069R, R1070Q, R1070W, F1074L, D1152H, G1244E, S1251N, S1255P, D1270N, and G1349D [L768, FDA Label]. When used in combination with the drug [DB09280] as the product Orkambi, ivacaftor is indicated for the management of CF patients age 6 years and older who are homozygous for the F508del mutation in the CFTR gene. |
| DB01764 | Dalfopristin | For the treatment of bacterial infections (usually in combination with quinupristin). |
| DB01369 | Quinupristin | For the treatment of bacterial infections (usually in combination with dalfopristin). |
| DB08827 | Lomitapide | Used in homozygous familial hypercholesterolemia (HoFH) patients to reduce low-density lipoprotein cholesterol (LDL-C), total cholesterol (TC), apolipoprotein B (apo B), and non-high-density lipoprotein cholesterol (non-HDL-C). |
| DB09073 | Palbociclib | Palbociclib is indicated in combination with [letrozole] as initial endocrine-based therapy for the treatment of human epidermal growth factor receptor type 2 (HER2)-negative and hormone receptor(HR)-positive tumors in adult patients with advanced/metastatic breast cancer. It is as well approved in combination with [fulvestrant] in patients with disease progression with prior endocrine therapy.[A176783] In the official labeling, the use of palbociclib should be accompanied with either an aromatase inhibition, no restricted to letrozole, as initial endocrine-based therapy in postmenopausal women or in man.[FDA label] The breast cancer starts as a group of cancer cells that grow into and destroy the nearby breast tissue. This growth can spread into other parts of the body which is called metastasis. According to the location of the cancer cells, it can be categorized in ductal carcinoma and lobular carcinoma. However, other types of breast cancer include inflammatory breast cancer, Paget disease of the breast, triple negative breast cancer non-Hodgkin lymphoma and soft tissue sarcoma.[L5870] In males, breast cancer is usually treated as the cases of postmenopausal women and almost all the cases are ductal carcinoma.[L5873] |
| DB06717 | Fosaprepitant | For the prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy. |
| DB09238 | Manidipine | For the treatment of hypertension. |
| DB11767 | Sarilumab | Indicated for modere to severe reactive RA in adult patients who are irresponsive, respond inadequately or present intolerance to disease-modifying anti-rheumatic drugs (DMARDs) or tumor necrosis factor (TNF) antagonists. It is indicated to be used in combination with methotrexate (MTX) or as a monotherapy when there is intolerance to MTX or MTX administration is inappropriate. |
| DB13941 | Piperaquine | For the treatment of uncomplicated *Plasmodium falciparum* infection in adults, children, and infants aged 6 months and up weighing over 5 kg [FDA Label]. Used in combination with [DB11638]. |
| DB12332 | Rucaparib | Indicated as monotherapy for the treatment of patients with deleterious BRCA mutation (germline and/or somatic) associated advanced ovarian cancer who have been treated with two or more chemotherapies. Select patients for therapy based on an FDA-approved companion diagnostic for rucaparib. |
| DB00501 | Cimetidine | For the treatment and the management of acid-reflux disorders (GERD), peptic ulcer disease, heartburn, and acid indigestion. |
| DB00921 | Buprenorphine | For the treatment of moderate to severe pain, peri-operative analgesia, and opioid dependence. |
| DB01173 | Orphenadrine | Indicated for the treatment of Parkinson's disease. |
| DB00188 | Bortezomib | For treatment of multiple myeloma in patients who have not been successfully treated with at least two previous therapies. |
| DB00289 | Atomoxetine | Atomoxetine is recommended for the treatment of attention deficit hyperactivity disorder (ADHD) in children and adults. It is recommended as a monotherapy in youths that do not respond correctly to stimulants.[A175723] ADHD is a neurodevelopmental disorder that can be categorized as a mental health condition. The symptoms of this condition start at childhood but they continue in adolescence and adulthood. The risk factors of ADHD are variable and they include the consumption of cigarettes, alcohol or drugs during pregnancy, low brain weight, brain injuries, toxical exposure or genetic disorders. The main symptoms for this condition are difficult in paying attention, overactivity and impulsivity.[L5665] |
| DB04839 | Cyproterone acetate | For the palliative treatment of patients with advanced prostatic carcinoma. |
| DB06791 | Lanreotide | Lanreotide is a somatostatin analog approved for treatment of neuroendocrine tumours and acromegaly. (2) |
| DB00104 | Octreotide | For treatment of acromegaly and reduction of side effects from cancer chemotherapy |
| DB06663 | Pasireotide | For the treatment of Cushing’s disease, specifically for those patients whom pituitary surgery has not been curative or is not an option. |
| DB09099 | Somatostatin | For the symptomatic treatment of acute bleeding from esophageal varices. Other treatment options for long-term management of the condition may be considered if necessary, once initial control has been established. |
| DB04894 | Vapreotide | For the treatment of esophageal variceal bleeding in patients with cirrhotic liver disease and has also shown efficacy in the treatment of patients with AIDS-related diarrhea. |
| DB11703 | Acalabrutinib | Acalabrutinib is currently indicated for the treatment of adult patients with Mantle Cell Lymphoma (MCL) who have received at least one prior therapy [FDA Label]. |
| DB05928 | Dovitinib | Investigated for use/treatment in multiple myeloma and solid tumors. |
| DB08864 | Rilpivirine | Rilpivirine, in combination with other agents, is indicated for the treatment of HIV-1 infections in antiretroviral treatment-naive patients with HIV-1 RNA ≤100,000 copies/mL and CD4+ cell count >200 cells/mm3.[L1030] The FDA combination therapy approval of rilpivirine and dolutegravir is indicated for adults with HIV-1 infections whose virus is currently suppressed (< 50 copies/ml) on a stable regimen for at least six months, without history of treatment failure and no known substitutions associated to resistance to any of the two components of the therapy.[L1031] |
| DB01128 | Bicalutamide | For treatment (together with surgery or LHRH analogue) of advanced prostatic cancer. |
| DB00215 | Citalopram | For the treatment of depression, as indicated by the FDA label [FDA label]. Off-label indications include but are not limited to: treatment of sexual dysfunction, post-stroke behavioural changes, ethanol abuse, obsessive-compulsive disorder (OCD) in children, and diabetic neuropathy [FDA label], [A321], [A322], [A323], [A324], [A174406], [A174409], [A174412]. |
| DB00476 | Duloxetine | For the acute and maintenance treatment of major depressive disorder (MDD), as well as acute management of generalized anxiety disorder. Also used for the management of neuropathic pain associated with diabetic peripheral neuropathy, and fibromyalgia. Has been used in the management of moderate to severe stress urinary incontinence (SUI) in women. |
| DB01175 | Escitalopram | Labeled indications include major depressive disorder (MDD) and generalized anxiety disorder (GAD). Unlabeled indications include treatment of mild dementia-associated agitation in nonpsychotic patients. |
| DB04884 | Dapoxetine | For the treatment of premature ejaculation. |
| DB01098 | Rosuvastatin | Used as an adjunct to dietary therapy to treat primary hyperlipidemia (heterozygous familial and nonfamilial), mixed dyslipidemia and hypertriglyceridemia. Also indicated for homozygous familial hypercholesterolemia as an adjunct to other lipid-lowering therapies or when other such therapies are not available. Furthermore, it is used to slow the progression of atherosclerosis and for primary prevention of cardiovascular disease. |
| DB01054 | Nitrendipine | For the treatment of mild to moderate hypertension |
| DB09078 | Lenvatinib | Lenvatinib is indicated for the treatment of patients with locally recurrent or metastatic, progressive, radioactive iodine-refractory differentiated thyroid cancer. |
| DB04920 | Clevidipine | For the treatment of hypertension. |
| DB00370 | Mirtazapine | For the treatment of major depressive disorder. |
| DB00455 | Loratadine | Loratadine is a 2nd generation antihistamine and is typically used to manage symptoms of allergic rhinitis, wheal formation and urticaria.[A176435][A176438] Unlike 1st generation antihistamines, loratadine is non-sedating since it has minimal effect on the central nervous system with only a small amount entering the brain. [A176438] |
| DB00778 | Roxithromycin | Used to treat respiratory tract, urinary and soft tissue infections. |
| DB01016 | Glyburide | Indicated as an adjunct to diet to lower the blood glucose in patients with NIDDM whose hyperglycemia cannot be satisfactorily controlled by diet alone. |
| DB04794 | Bifonazole | Used for the treatment of various topical fungal infections, including athlete's foot (tinea pedis). |
| DB00898 | Ethanol | For therapeutic neurolysis of nerves or ganglia for the relief of intractable chronic pain in such conditions as inoperable cancer and trigeminal neuralgia (tic douloureux), in patients for whom neurosurgical procedures are contraindicated. |
| DB01321 | Josamycin | For the treatment of bacterial infections. |
| DB00316 | Acetaminophen | In general, acetaminophen is used for the treatment of mild to moderate pain and reduction of fever [F4124]. It is available over the counter in various forms, the most common being oral forms. Acetaminophen _injection_ is indicated for [FDA label]: • Management of mild to moderate pain • Management of moderate to severe pain with adjunctive opioid analgesics • Reduction of fever Because of its low risk of causing allergic reactions, this drug can be administered in patients who are intolerant to salicylates and those with allergic tendencies, including bronchial asthmatics [F4124]. Specific dosing guidelines should be followed when administering acetaminophen to children [L5780]. |
| DB02701 | Nicotinamide | Not Available |
| DB00763 | Methimazole | For the treatment of hyperthyroidism, goiter, Graves disease and psoriasis. |
| DB09036 | Siltuximab | Siltuximab is indicated for the treatment of patients with multicentric Castleman's disease (MCD) who are human immunodeficiency virus (HIV) negative and human herpesvirus-8 (HHV-8) negative. Siltuximab did not bind to virally produced IL-6 in a nonclinical study and was therefore not studied in patients with MCD who are HIV or HHV-8 positive. |
| DB09063 | Ceritinib | Ceritinib is a kinase inhibitor indicated for the treatment of patients with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC) who have progressed on or are intolerant to crizotinib. This indication is approved under accelerated approval based on tumor response rate and duration of response. An improvement in survival or disease-related symptoms has not been established. Continued approval for this indication may be contingent upon verification and description of clinical benefit in confirmatory trials. |
| DB09330 | Osimertinib | Osimertinib is indicated for the treatment of patients with metastatic epidermal growth factor receptor (EGFR) T790M mutation-positive non-small cell lung cancer (NSCLC), as detected by an FDA- approved test, who have progressed on or after EGFR-TKI therapy. |
| DB00864 | Tacrolimus | For use after allogenic organ transplant to reduce the activity of the patient's immune system and so the risk of organ rejection. It was first approved by the FDA in 1994 for use in liver transplantation, this has been extended to include kidney, heart, small bowel, pancreas, lung, trachea, skin, cornea, and limb transplants. It has also been used in a topical preparation in the treatment of severe atopic dermatitis. |
| DB01234 | Dexamethasone | Injection: for the treatment of endocrine disorders, rheumatic D=disorders, collagen diseases, dermatologic diseases, allergic statesc, ophthalmic diseases, gastrointestinal diseases, respiratory diseases, hematologic disorders, neoplastic diseases, edematous states, cerebral edema.
Ophthalmic ointment and solution: for the treatment of steroid responsive inflammatory conditions of the palpebral and bulbar conjunctiva, cornea, and anterior segment of the globe. Ophthalmic solution only: for the treatment of steroid responsive inflammatory conditions of the external auditory meatus Topic cream: for relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses Oral aerosol: for the treatment of bronchial asthma and related corticosteroid responsive bronchospastic states intractable to adequate trial of conventional therapy Intranasal aerosol: for the treatment of allergic ot inflammatory nasal conditions, and nasal polyps |
| DB09074 | Olaparib | Olaparib is a poly (ADP-ribose) polymerase (PARP) inhibitor indicated for the treatment of: (I) Ovarian cancer, in which the medication is intended for [a] the maintenance treatment of adult patients with recurrent epithelial ovarian, fallopian tube or primary peritoneal cancer, who are in complete or partial response to platinum-based chemotherapy, or [b] for the treatment of adult patients with deleterious or suspected deleterious germline BRCA-mutated (gBRCAm) advanced ovarian cancer who have been treated with three or more prior lines of chemotherapy [FDA Label]. Select patients for therapy based on an FDA-approved companion diagnostic for olaparib [FDA Label]. [II] Breast cancer, in which the medication is intended for use in patients with deleterious or suspected deleterious gBRCAm, human epidermal growth factor receptor 2 (HER2)-negative metastatic breast cancer who have previously been treated with chemotherapy in the neoadjuvant, adjuvant or metastatic setting. Patients with hormone receptor (HR)-positive breast cancer should have been treated with a prior endocrine therapy or be considered inappropriate for endocrine treatment [FDA Label]. Select patients for therapy based on an FDA-approved companion diagnostic for olaparib [FDA Label]. |
| DB00091 | Ciclosporin | Cyclosporine is officially approved for different conditions listed below: * Prophylaxis of organ rejection in kidney, liver, and heart allogeneic transplants. For this indication, it can be used concomitantly with azathioprine and corticosteroids. * Treatment of patients with severe active, rheumatoid arthritis when the patient no longer responds to methotrexate. * Concomitantly with methotrexate for the treatment of patients with severe active rheumatoid arthritis when patients do not respond to methotrexate treatment alone. * Treatment of adult nonimmunocompromised patients with severe, recalcitrant, plaque psoriasis that have failed to respond to at least one systemic therapy or when systemic therapies are not tolerated or contraindicated.[FDA label] * Its ophthalmic solution is indicated to increase tear production in patients with keratoconjunctivitis sicca in patients from 4 years old.[L5158] * Prevention of graft rejection following bone marrow transplantation and in the treatment of graft-versus-host disease (GVHD). * Treatment of steroid dependent and steroid-resistant nephrotic syndrome due to glomerular diseases such as minimal change nephropathy, focal and segmental glomerulosclerosis or membranous glomerulonephritis in adults and children.[F3091] Away from all this approved and reviewed indications, cyclosporine is commonly used on dermatology for the treatment of various inflammatory skin conditions such as atopic dermatitis, blistering disorders, and connective tissue diseases.[A174085] |
| DB00243 | Ranolazine | Ranolazine is approved as a second-line agent in the management of chronic stable angina pectoris that is refractory to conventional anti-ischemic therapy.[A174913] Ranolazine has also been used off-label for the treatment of some arrhythmias such as ventricular tachycardia, however, this use does not have a lot of supporting evidence.[A174940] The use of ranolazine has been researched in the treatment of acute coronary syndrome, microvascular coronary dysfunction, arrhythmia, and glycemic control.[A174898] |
| DB00334 | Olanzapine | Olanzapine was initially used orally and intramuscularly for the chronic treatment of schizophrenia in patients over 13 years old and other psychiatric disorders such as bipolar I disorder including mixed or manic episodes.[A177014] Olanzapine is also indicated, in combination with lithium or valproate for the short-term treatment of acute manic or mixed episodes associated with bipolar I disorder in adults.[FDA label] As well, olanzapine is indicated, in combination with fluoxetine for the treatment of episodes of depression associated with bipolar disorder type 1 and treatment-resistant depression in patients over 10 years old.[A177014] Olanzapine is also approved for the management of psychomotor agitation associated with schizophrenia and bipolar I mania.[FDA label] Schizophrenia is a complex biochemical brain disorder that affects the person's ability to differentiate reality. It is usually observed as the presence of delusions, hallucinations, social withdrawal and disturbed thinking.[L5936] Bipolar disorder is a mental health condition defined by periods of extreme mood disturbances. It is categorized in different types from which type 1 is known to involve episodes of severe mania and often depression while type 2 presents less severe forms of mania.[L5939] |
| DB00863 | Ranitidine | This drug is used alone or with concomitant antacids for the following conditions [FDA label]: **Duodenal ulcer** Treatment of active duodenal ulcer (short-term), maintenance therapy of duodenal ulcers after healing (reduced dose) **Pathological hypersecretion of gastric acid** Zollinger-Ellison syndrome, systemic mastocytosis, and other conditions causing gastric acid hypersecretion **Gastric ulcer** Short term treatment of active gastric ulcer (benign), maintenance of healing after gastric acid ulcer therapy (reduced dose) **Other conditions**: Treatment of GERD symptoms (symptoms usually improve within 24 hours), treatment of erosive esophagitis (endoscopically diagnosed) and maintenance of healing [FDA label] |