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What are the targeted drugs for breast cancer?

What are the targeted drugs for breast cancer?

Cancer systemic drug therapy is no longer the era of chemotherapy to fight the world, targeted drugs occupy an important position, and nowadays, we are entering the era of immunotherapy. This question is asking what are the targeted drugs for breast cancer'?

Targeted drugs for breast cancer can be categorized into the following broad groups:

The first category is targeted anti-hematopoietic agents, such as bevacizumab (Avastin), which are considered in certain cases but are of little value in breast cancer.

The second category is anti-HER-2 targeted drugs, which is the most important targeted drug for breast cancer and the core drug (of course, for HER-2 positive patients), including the main drugs trastuzumab (Herceptin), patuximab, TDM-1, lapatinib, and so on.

The third category is for patients with BRCA germline mutations, and the primary drug is olaparib, which is used to treat patients with metastatic breast cancer who have a deleterious, or are suspected to have a deleterious, germline BRCA mutation with human epidermal growth factor receptor 2 (HER2)-negative metastatic breast cancer.

The fourth category is actually immunotherapeutic drugs, that is, anti-PD-1/PD-L1 monoclonal antibodies, which are also considered targeted drugs in a sense, but essentially unleash immunosuppression and activate immune cells to kill cancer cells.

The above are the main targeted drugs for breast cancer, and there are still in the clinical trial stage, I believe there will be more and more targeted drugs come out in the future to benefit more breast cancer patients, look forward to it together.

Targeted therapy is a major component of precision medicine, which targets genetic changes in cancer cells that can help them grow, divide and spread. Drugs entering the body will specifically bind to the targets of cancer cells to have an effect, causing tumor cells to die specifically without affecting the normal tissue cells around the tumor, so molecular targeted therapy is also known as "biological missiles".



HER-2 targets

For breast cancer the more mature target of current research is the HER-2 gene, HER-2 gene, mainly induces tumor generation. Targeted drugs mainly inhibit the growth of tumor cells by binding with HER-2.trastuzumabThat is, Herceptin is a more familiar targeted drug that has entered the Medicare category.

Lapatinib:Lapatinib is a brand new targeted drug after trastuzumab, which can effectively inhibit intracellular EGFR (erbB-1) and HER-2 (erbB-2) ATP sites to prevent tumor cell phosphorylation and activation. it was approved by FDA for marketing in March 2007, and is now available for purchase in China.



T-DM1:is an antibody-drug coupling. Through a software linkage, the coupling combines the targeted anti-tumor properties of expectorant bead monoclonal antibody with the cytotoxic effects of the microtubule inhibitor DM1. As an antibody-drug conjugate, T-DM1 retains the targeting properties of sole monoclonal antibody against HER-2 positive breast cancer, but carries a potent cytotoxic drug (DM1) into tumor cells to inhibit microtubule protein polymerization and microtubule dynamics.



Pertuzumab:It mainly acts on HER-2 receptor proteins, and studies have shown that trastuzumab in combination with patuzumab improves efficacy and has a therapeutic effect on trastuzumab-resistant patients.

Everolimus:A targeted therapeutic agent located downstream of the HER-2 receptor, everolimus has been reported in studies to overcome primary resistance to trastuzumab.

VEGF targets

Inhibition of angiogenic factor (VEGF) bevacizumab: To block the biological effects of VEGF by neutralizing VEGF, thereby inhibiting the formation of neovascularization and reducing the supply of oxygen, blood and other nutrients to the tumor area, thereby inhibiting tumor growth. Studies have shown that in metastatic ductal carcinoma and triple-negative breast cancer, the level of VEGF is significantly elevated. Therefore, the use of tetanizumab is effective. It has been confirmed by a large number of clinical trials.



VEGFR tyrosine kinase inhibitor sorafenib, also blocking the angiogenic effects of VEGF.

The mTOR inhibitor everolimus:

Endocrine and growth factor receptors in breast cancer activate mTOR through the PI3K/Akt pathway, and inhibition of mTOR can potentially interfere with multiple dimensions of breast cancer. Everolimus has been used in hormone receptor-positive breast cancer, HER-2 breast cancer and triple-negative breast cancer.

Targeting DNA Damage Drugs

Primarily for patients with BRCA mutations. Primarily a PARP (Poly Adenosine Diphosphate Ribose Polymerase) inhibitor that enhances chemotherapy-mediated DNA damage.On January 12, 2018, the FDA approved Olaparib, a Poly ADP-ribose Polymerase (PARP) inhibitor, for use in BRCA-mutated HER2 negative metastatic breast cancer, opening up another horizon for targeted breast cancer therapy.



These are the more well-studied targets and drugs, and there are many new drugs as well as clinical trials underway and advancing. Today the Breast Cancer Conference San Antonio is publicizing the results of studies on dual target therapy with patulin and trastuzumab. In other words, everything is hopeful and the new drugs are worth waiting for.

Thank you for your question.

(1) Breast cancer medication:

Two novel targeted agents are recommended: trastuzumab (injectable) and lapatinib tosylate tablets (oral);

1) Trastuzumab injection: indications: can be used for recurrent metastatic breast cancer, can be combined with chemotherapeutic drugs such as paclitaxel or docetaxel; adjuvant treatment for breast cancer, can be combined with chemotherapeutic drugs such as paclitaxel and cyclophosphamide; neoadjuvant treatment for breast cancer; before receiving trastuzumab treatment, firstly, the HER2 test is carried out, and HER2-positive patients can be treated with trastuzumab; studies show that HER2-positive metastatic breast cancer patients can be treated with trastuzumab in combination with other chemotherapeutic drugs to enhance the therapeutic effect;

2) Lapatinib tosylate tablets:

Lapatinib tosylate is used in combination with capecitabine for the treatment of patients with advanced or metastatic breast cancer;

This product can be used alone, 1.25 g once daily for days 1-21 consecutively. Take at least 1 hour before or at least 1 hour after a meal; Capecitabine, recommended dose 2g/(m2.day) in two divided doses, 12 hours apart, for 14 days, with a 7-day rest period, for a 21-day cycle, can be taken with food or 30 minutes after a meal;

Lapatinib tosylate its main adverse reactions: diarrhea and rash, diarrhea can be treated with symptomatic treatment, avoid sun exposure during the medication period, go out and pay attention to sun screen; this product is mainly metabolized by CYP3A4, during the medication period, forbidden to eat grapefruit and grapefruit juice. If you miss a dose on a particular day while taking it, you do not need to double it on the next day, just continue to take it according to the original schedule;

I hope you find it helpful!

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Breast cancer is the number one killer threatening women's health, with the risk exceeding that of cervical cancer. Mainly affected by life stress as well as hereditary genes, the number of women suffering from the disease has been increasing in recent years, and should not be ignored.

Breast cancer focuses on early detection

Breast is not an important gland in the body. Early breast cancer will not affect the health of the body because of the dense deconstruction, as long as timely surgery to get rid of it. However, if the breast cancer cells are afraid of shedding in the later stage, the free cancer cells can go with the blood to every corner of the body, and take root in other parts of the body or develop in the lymphatic area, and the consequences cannot be underestimated. 2000 years later, the mortality rate of breast cancer has dropped a lot, mainly due to the early detection and breakthroughs in the treatment of breast cancer, and nowadays, there is no danger to the life of the early stage breast cancer, and the cure rate is very high with targeted drugs, surgical excision and other means. Nowadays, early breast cancer is basically not life-threatening, and with targeted drugs, surgical resection and other means, the cure rate is very high, and it has become one of the several solid tumors with the best therapeutic effect.

Early Symptoms of Breast Cancer

If you want to treat it, you must do it early. So what are the symptoms of early onset breast cancer?

①Lump in the breast

A lump in this context refers to a breast lump and 80% of breast cancers in women are detected due to the presence of a lump. It can be felt with a light touch and most of the lumps are painless, a few some have a tingling sensation.

② Nipple overflow

When the nipple secretion of milk, blood, juice, pus, etc. occurs during non-pregnancy, it should be taken seriously enough. Even if it is not the cause of breast cancer, it may be nipple tumor, breast hyperplasia and other problems, early detection should be treated, so as not to seriously spend more energy and money later.

③Cellulite lines near the breasts

Whether men or women, when the breast near the "orange peel-like lines" is not a good sign, must cause enough vigilance, because the risk of breast cancer at this time has been as high as 90%, mainly cancerous tumors cut off the muscle tissues and ligaments, resulting in atrophy of the skin, when the skin pits or folds, you should immediately go to the examination. When skin pits or folds appear, you should go for checkup immediately.

When you notice something strange in your body, go for a checkup right away. Hospitals have a variety of methods such as mammograms, overflow analysis, puncture sampling and other means to confirm the diagnosis, which are extremely convenient and inexpensive.

Treatment of breast cancer

The vast majority of breast cancer will take radical resection surgery, after the removal of the lesion through targeted drugs or radiotherapy for further treatment, traditional Chinese medicine to control and regulate the body, hormone control and other means of this series of treatment.

Among other things, mastectomy is no longer something that makes people sad and upset, and doctors can perform protective excision and later restore the breast as a whole through autograft reconstruction and other maneuvers that do not make women sad.

Targeted drugs for the treatment of breast cancer include pabocinib, T-DM1, patuximab, trastuzumab, lapatinib, and everolimus.

Targeted drugs are mainly used for the treatment of a small proportion of breast cancer gene HER2 positive used, more representative of palatinib and trastuzumab. Targeted therapy is usually practiced after surgery when the HERB-2 receptor is found to be three plus signs or more.

Breast cancer nowadays can not do as simple treatment as a cold and fever, but now has been removed from the situation of certain death of cancer, as long as it has not spread, basically can be cured, unless the luck is really bad, many local hospitals can be treated, do not be afraid, as long as you adhere to the improvement of the diet, change the time of rest and relaxation, and strengthen the exercise, breast cancer can be said to go bye-bye.

Men are also at risk of breast cancer, so appeal symptoms if they occur in men as well, must also be dietary attention. Like please follow me, every day to push interesting and knowledgeable articles to you!

Targeted therapeutic drugs for breast cancer include trastuzumab, patuximab, lapatinib, afatinib and many other drugs, and the best drug is selected for treatment according to the condition. Some drugs often cause obvious digestive discomfort, such as nausea, vomiting, diarrhea, loss of appetite and other symptoms, which usually do not affect normal life, and if the adverse reaction of the drug continues to worsen, it is necessary to be admitted to the hospital to consult the doctor to adjust the type of drug or change the dosage of the drug under the doctor's guidance. If the adverse effects of the drug continue to worsen, it is necessary to go to the hospital and adjust the type of drug or change the dosage of the drug under the guidance of the doctor.

Breast cancer patients have firm beliefs in the treatment process, keep optimistic life attitude and overcome the disease. Family members of the patients do a good job in psychological support, and find that the patients are in a relatively low state, and are timely psychological counseling.

Currently it is trastuzumab is now considered a basic drug, most of the others are not listed domestically, and the domestic patrozumab is used as a second-line drug.

The most complete list of targeted breast cancer drugs and their side effects is here:

Breast cancer is the leading cause of cancer deaths in women worldwide. For the treatment of breast cancer, targeted drugs have received more and more attention. Countless breast cancer patients are looking forward to better treatment results.

In addition to the effectiveness of the treatment, many cancer patients are also very concerned about how the side effects of these drug treatments will be.

Let's take a look at what exactly are the side effects of targeted breast cancer treatment drugs? After all, it's better to know what you're getting into than what you're getting out of.

Lapatinib (Telisha)

Lapatinib in combination with capecitabine is indicated for the treatment of HER2 overexpressing advanced or metastatic breast cancer previously treated with anthracycline, paclitaxel and trastuzumab.

Most common adverse reactions (≥20%)

Diarrhea, erythema on palms-sole of feet, nausea, rash, vomiting and fatigue.

Lapatinib in combination with letrozole is indicated for the treatment of metastatic postmenopausal breast cancer with hormone receptor-positive, HER2 overexpression.

Most common adverse reactions (≥20%)

Diarrhea, rash, nausea and fatigue.

Trastuzumab (Herceptin)

complementary therapy

Trastuzumab is indicated for the adjuvant treatment of HER2 overexpressing, lymph node-positive or -negative (ER/PR-negative or with one high-risk feature) breast cancer.

As part of a regimen that includes adriamycin, cyclophosphamide, paclitaxel or doxorubicin

As part of a regimen of doxorubicin and carboplatin

as a single agent for subsequent multimodal anthracycline-based therapy

Most common adverse reactions (≥5%)

Headache, diarrhea, nausea and chills.

metastatic breast cancer

Trastuzumab in combination with paclitaxel is indicated for the first-line treatment of HER2 overexpressing metastatic breast cancer.

Trastuzumab is indicated as a single agent for the treatment of HER2 overexpressing metastatic breast cancer that has received one or more prior chemotherapy regimens.

Most common adverse reactions (≥10%)

Fever, chills, headache, infections, congestive heart failure, insomnia, cough and rash.

(T-DM1) Kadcyla

T-DM1 is indicated as a single agent for the treatment of HER2-positive metastatic breast cancer previously treated with trastuzumab and paclitaxel alone or in combination.

These patients should have received prior treatment for metastatic disease or have had a recurrence of disease during or within six months of completing adjuvant therapy.

Most common adverse reactions (>25%)

Fatigue, nausea, musculoskeletal pain, bleeding, thrombocytopenia, headache, elevated transaminases, constipation, and nosebleeds.

Pertuzumab (Perjeta)

metastatic breast cancer

Pertuzumab in combination with trastuzumab and doxorubicin is indicated for the treatment of HER2-positive metastatic breast cancer that has not received prior anti-HER2 therapy or chemotherapy.

Most common adverse reactions (>30%)

Diarrhea, alopecia, neutropenia, nausea, fatigue, rash and peripheral neuropathy.

Neoadjuvant therapy for early breast cancer

Pertuzumab in combination with trastuzumab and chemotherapy is indicated for neoadjuvant treatment of HER2-positive, locally advanced, inflammatory, or early-stage breast cancer (greater than 2 cm in diameter or lymph node-positive) as part of a complete treatment regimen for early-stage breast cancer.

Pertuzumab in combination with trastuzumab and doxorubicin

Most common adverse reactions (>30%)

Alopecia, diarrhea, nausea and neutropenia.

Continuation of a 3-cycle FEC (fluorouracil, epirubicin, cyclophosphamide) regimen followed by 3 cycles of patuzumab in combination with trastuzumab and doxorubicin

Most common adverse reactions (>30%)

Fatigue, hair loss, diarrhea, nausea, vomiting and neutropenia.

Pertuzumab in combination with doxorubicin, carboplatin and trastuzumab (TCH)

Most common adverse reactions (>30%)

Fatigue, hair loss, diarrhea, nausea, vomiting, neutropenia, thrombocytopenia and anemia.

Continuation of a 4-cycle ddAC (dose-dense adriamycin and cyclophosphamide) regimen followed by 4 cycles of patuximab in combination with trastuzumab and paclitaxel

Most common adverse reactions (>30%)

Nausea, diarrhea, hair loss, fatigue, constipation, peripheral neuropathy and headaches.

Continuation of a 4-cycle FEC (fluorouracil, epirubicin, cyclophosphamide) regimen followed by 4-cycle patuzumab in combination with trastuzumab and doxorubicin

Most common adverse reactions (>30%)

Diarrhea, nausea, alopecia, weakness, constipation, fatigue, inflammation of mucous membranes, vomiting, myalgia and anemia.

Adjuvant therapy for early breast cancer

Pertuzumab in combination with trastuzumab and chemotherapy is indicated as adjuvant therapy for HER2-positive early breast cancer with a high risk of recurrence.

Most common adverse reactions (>30%)

Diarrhea, nausea, hair loss, fatigue, peripheral neuropathy and vomiting.

Lenatinib (Nerlynx)

Indicated for the treatment of HER2-positive early breast cancer previously treated with trastuzumab.

Most common adverse reactions (>5%)

Diarrhea, nausea, abdominal pain, fatigue, vomiting, rash, stomatitis, decreased appetite, muscle cramps, dyspepsia, elevated AST or ALT, NAIL DISORDER, dry skin, bloating, weight loss and urinary tract infections.

Pabosini (Ibrance)

Pabocinib in combination with an aromatase inhibitor is indicated as initial endocrine therapy for hormone receptor-positive, HER2-negative advanced or metastatic postmenopausal breast cancer.

Pabocinib in combination with fulvestrant is indicated for the treatment of hormone receptor-positive, HER2-negative advanced or metastatic breast cancer with disease progression after endocrine therapy.

Most common adverse reactions (≥10%)

Neutropenia, infections, leukopenia, fatigue, nausea, stomatitis, anemia, alopecia, diarrhea, thrombocytopenia, rash, vomiting, loss of appetite, weakness and fever.

Rebosini (Kisqali)

Rebocinib in combination with an aromatase inhibitor is indicated as initial endocrine therapy for hormone receptor-positive, HER2-negative locally advanced or metastatic postmenopausal breast cancer.

Most common adverse reactions (≥10%)

Urinary tract infection, neutropenia, leukopenia, anemia, lymphopenia, decreased appetite, headache, insomnia, dyspnea, nausea, diarrhea, vomiting, constipation, stomatitis, abdominal pain, alopecia, rash, itching, back pain, fatigue, peripheral edema, weakness, fever, abnormal liver function tests.

Common adverse reactions (1-10%)

Thrombocytopenia, febrile neutropenia, hypocalcemia, hypokalemia, hypophosphatemia, increased lacrimation, dry eye, syncope, rhinorrhea, dysgeusia, dyspepsia, hepatotoxicity, erythema, increased blood creatinine, weight loss, and prolonged ECG QT.

Goserelin (Noladex)

Indicated as palliative treatment for advanced premenopausal and perimenopausal breast cancer that is hormone receptor positive.

Adverse reactions (>20%)

Hot flashes, headaches, sweating, acne, emotional instability, depression, decreased libido, vaginitis, breast atrophy, seborrhea, and peripheral edema. In addition, tumor bulge growth occurs during the initial phase of goserelin treatment.

Everolimus (Fenitol)

Everolimus in combination with exemestane is indicated for the treatment of hormone receptor-positive, HER2-negative advanced postmenopausal breast cancer that has failed both treatment with letrozole or anastrozole.

Most common adverse reactions (≥30%)

Stomatitis, infections, rashes, fatigue, diarrhea, edema, abdominal pain, nausea, fever, weakness, cough, headache and loss of appetite.

Abemaciclib (Verzenio)

Abemaciclib in combination with an aromatase inhibitor is indicated as initial endocrine therapy for hormone receptor-positive, HER2-negative advanced or metastatic postmenopausal breast cancer.

Abemaciclib in combination with fulvestrant is indicated for the treatment of hormone receptor-positive, HER2-negative advanced or metastatic breast cancer with disease progression after endocrine therapy.

Abemaciclib is indicated as a single agent for the treatment of hormone receptor-positive, HER2-negative advanced or metastatic breast cancer that has progressed after receiving chemotherapy in endocrine therapy and metastatic disease treatment regimens.

Most common adverse reactions (≥20%)

Diarrhea, neutropenia, nausea, abdominal pain, infections, fatigue, anemia, leukopenia, loss of appetite, vomiting, headache, hair loss, and thrombocytopenia.

Tamoxifen

Indicated for the treatment of recurrent metastatic breast cancer in women.

It is indicated as an adjuvant treatment for metastasis after breast cancer surgery to prevent recurrence.

Bone and tumor pain may be transiently aggravated at the beginning of the treatment and may be gradually reduced with continued treatment. A few patients have adverse reactions.

Among them, gastrointestinal reactions: loss of appetite, nausea, vomiting, diarrhea. Reproductive system: menstrual disorders, amenorrhea, vaginal bleeding, vulvar itching, endometrial hyperplasia, endometrial polyps and endometrial cancer. Skin: flushing of the face, rash, alopecia. Bone marrow: occasional leukopenia and thrombocytopenia. Occasional abnormal liver function. Eyes: Retinopathy or corneal clouding may occur with prolonged (17 months or more) use of large amounts (240-320 mg daily). Rare adverse reactions of concern: confusion, pulmonary embolism (manifested by shortness of breath), thrombosis, weakness, drowsiness.

Anastrozole (Raninde)

Indicated as adjuvant therapy for hormone receptor-positive early postmenopausal breast cancer.

Indicated as first-line treatment for locally advanced or metastatic postmenopausal breast cancer with positive or unknown hormone receptors.

Indicated as second-line treatment for advanced postmenopausal breast cancer with disease progression following tamoxifen therapy.

ER-negative and previously ineffective tamoxifen-treated patients also rarely respond to anastrozole.

Most common adverse reactions in early breast cancer (≥10%)

Hot flashes, weakness, arthritis, aches and pains, arthralgia, pharyngitis, hypertension, depression, nausea and vomiting, skin rashes, osteoporosis, bone fractures, back pain, insomnia, headaches, peripheral edema and lymphedema.

Most common adverse reactions in advanced breast cancer (>10%)

Hot flashes, nausea, weakness, aches and pains, headaches, back pain, bone pain, worsening cough, dyspnea, pharyngitis and peripheral edema.

Letrozole (Flon)

Indicated as adjuvant therapy for hormone receptor-positive early postmenopausal breast cancer.

Indicated as extended adjuvant therapy for early postmenopausal breast cancer that has received 5 years of adjuvant tamoxifen therapy.

Indicated as first-line treatment for locally advanced or metastatic postmenopausal breast cancer with positive or unknown hormone receptors.

Indicated for the treatment of advanced postmenopausal breast cancer with disease progression following anti-estrogen therapy.

Most common adverse reactions (>20%)

Hot flashes, arthralgia, flushing, weakness, edema, arthralgia, headache, dizziness, hypercholesterolemia, increased sweating, bone pain, and pain or stiffness at the musculoskeletal area.

Olapani (Lipitor)

Indicated for the treatment of HER2-negative metastatic breast cancer harboring a germline BRCA mutation (deleterious or suspected deleterious) that has received chemotherapy in the prior treatment regimen for neoadjuvant, adjuvant, or metastatic disease.

Patients with hormone receptor-positive breast cancer should be prioritized for endocrine therapy.

(Currently, olaparib is only approved for the maintenance treatment of platinum-sensitive recurrent ovarian cancer in China, regardless of whether the patient carries a BRCA gene mutation).

Most common adverse reactions in clinical trials (≥20%)

Anemia, nausea, fatigue (including weakness), vomiting, neutropenia, leukopenia, nasopharyngitis/upper respiratory infection/flu, respiratory infections, diarrhea, arthralgia/myalgia, dysgeusia, headache, dyspepsia, loss of appetite, constipation and stomatitis.

Most common abnormalities in the laboratory (≥25%)

Decreased hemoglobin, increased mean red cell volume, decreased lymphocytes, decreased leukocytes, decreased absolute neutrophil count, increased serum creatinine and thrombocytopenia.

Talazoparib (Talzenna)

Indicated for the treatment of locally advanced or metastatic breast cancer carrying a germline BRCA mutation (deleterious or suspected deleterious) and HER2-negative.

Most common adverse reactions (≥20%)

Fatigue, anemia, nausea, neutropenia, headache, thrombocytopenia, vomiting, hair loss, diarrhea, loss of appetite.

Most common abnormalities in the laboratory (≥25%)

Decreased hemoglobin, platelets, neutrophils, lymphocytes, leukocytes and calcium. Glucose, alanine aminotransferase, aspartate aminotransferase and alkaline phosphatase are increased.

Above, we have compiled relevant information about the side effects of targeted breast cancer drugs for you, and we hope it will be helpful to you. It is important to note that you should never stop taking the medication or refuse treatment because of the side effects of the medication, and you should always communicate with your treating doctor.

Piratinib, a newly approved targeted drug for breast cancer, is a new generation of targeted drug for anti-HER2 therapy, which is more comprehensive in targeting, more bioavailable, and more potent in inhibiting tumor growth compared with the previous generation of anti-HER2 drugs, such as trastuzumab, lapatinib, lenatinib, and so on. Olaparib can also be used if, for example, a breast cancer patient carries a deleterious mutation in the BRCA germline. This drug has been approved by the FDA for the treatment of metastatic breast cancer patients who carry a deleterious germline mutation of BRCA and are HER2-negative. It is also a new boon for HER2-negative breast cancer patients for whom anti-HER2 drugs such as trastuzumab and lapatinib are not effective.

Before we answer that question, let's understand what exactly is meant by targeted therapy.

In terms of medical theory, the so-called targeting is to use molecular targeting drugs to inhibit these targets, thereby blocking tumor cell signaling and nutrient transmission, so as to achieve the inhibition or killing of tumor cells. However, this target is not easy to find, which involves the difference in genetic expression between normal human cells and tumor cells, and it is this difference that can be used as a target.

So far, of course, targeted therapy for breast cancer in individual cancer foci has been found to have an effective target both"Human Epidermal Growth Factor Receptor 2"... that's a mouthful, isn't it? It's also known as HER2.

The application of molecular targeting research to breast cancer again requires the classification of breast cancer into three categories:

In the first category, estrogen-dependent type of breast cancer, such patients are only suitable for endocrine therapy.

In the second category, which is what we call genetically inherited abnormal breast cancer above, or HER2-positive breast cancer, such patients are more suitable for targeted drug therapy.

The third category, triple-negative breast cancer, which is the presence of both of the above conditions, both estrogen-dependent and HER2, is more complex and is usually treated with chemotherapy.

Patients are diagnosed by immunohistochemical testing (IHC testing) with fluorescence in situ hybridization. If the IHC test result is ++++,then it is certain that the patient is a HER2 positive breast cancer patient and suitable for targeted therapy. However, if the IHC test is +,or ++, then in this case, FISH is also needed to confirm the diagnosis.

In HER2-positive targeted drug therapy for breast cancer, common drugs aretrastuzumab.This is a targeted drug that acts selectively on the outside of HER2 cells;Lapatinib, an orally targeted inhibitor of small molecule tyrosine kinases, primarily against HER1 and HER2;Pertuzumab, this drug is a recombinant monoclonal that inhibits dimer formation and inhibits receptor-mediated signaling pathways;NeratinibIt is an oral tyrosine kinase inhibitor that irreversibly inhibits EGFR, HER2, and HER4;afatinibis an orally available small molecule drug with irreversible inhibition of HER1, 2 and 4.

It is important to note that while targeted drugs can control breast cancer to a certain extent, there is also the possibility of developing resistance, which appears perhaps six months, or a year, after treatment. When the drug becomes resistant, it means that it has lost its effect. This is the time to change the treatment program.

How to extend the targeted drug resistance is particularly important, many medical practitioners and their families are actively looking for ways, but most of the cases can only assist or alleviate. At present, some medical practitioners pointed out the use of traditional Chinese medicine to improve, including ginsenoside rh2, ganoderma lucidum powder, ginsenoside powder, panax ginseng powder, etc., can be in certain conditions to assist in prolonging the resistance to targeted drugs, improve the human body's immune resistance to help inhibit the tumor cells and prevent recurrence and metastasis.

Welcome to the anti-cancer health network: What are your different opinions on this issue? Welcome to leave a comment below, don't forget to give the anti-cancer health network point a praise oh~!

The question, which can be somewhat controversial to answer, is whether the hormonal factors (estrogen ER and progesterone PR) that contribute most to the development of breast cancer are drug targets?

These two hormonal factors are completely different from the EGFR, ALK, MET, ROS1, etc. that you often see in lung cancer, and the HER2 targets in the same breast cancer, where a clear location of the mutation can be found; while ER and PR simply lead to changes in hormone levels.

However, in the treatment many oncologists believe that drugs against hormone receptor positive drugs can also be counted as targeted drugs, for example: tamoxifen, letrozole, anastrozole, toremifene and so on can be counted as targeted drugs.

In addition to hormone inhibiting drugs, the division for other targeted drugs for breast cancer is relatively uniform, according to different targets or drug properties are divided into the following five categories:

Drugs targeting HER2 overexpression:

Trastuzumab (Herceptin), patuximab, lapatinib, pyrrolitinib and T-DM1 (Kadcyla) drugs. The first four of these are already available in China. Piratinib belongs to the dual-targeting drugs of HER2 and EGFR, and is approved in China for the treatment of HER2-positive patients with advanced breast cancer cancer in combination with capecitabine.

The criteria for determining HER2 overexpression need to be clarified: first look at the immunohistochemistry IHC results, if the HER2 is already 3+ or more, it is clear that the corresponding drugs can be used; if there is no or only one +, it does not belong to HER2 overexpression, and the use of this kind of drugs is invalid; if there are exactly 2 +, then it is necessary to supplement the FISH genetic testing. The results of FISH are positive and negative. Positive results allow the use of HER2-targeting drugs, while negative results do not require their use.

Lapatinib is a small molecule oral drug, which is easy to use, with fast onset of action and few side effects. Lapatinib is well tolerated orally, can cross the blood-brain barrier, combined with chemotherapy for breast cancer brain metastasis patients with better efficacy.

The T-DM1 drug is an antibody-coupled drug, specifically trastuzumab-emtansine; an antibody-coupled drug of a targeted agent (Herceptin) and the chemotherapeutic agent medenosine (a chemotherapeutic agent that inhibits microtubule aggregation), so it can be both HER2-targeted and chemo-killed.

Targeted anti-angiogenic drugs

Vascular endothelial growth factor (VEGF) is a key factor in angiogenesis, blood vessels near the tumor can help form the tumor microenvironment, more access to nutrients for rapid growth. Therefore, there are anti-vascular inhibitory targeted drugs targeted drugs, this kind of drugs belong to the cancer treatment in the "oil of gold", in the kind of cancer treatment are used. Specific drugs include sorafenib, regrafenib, lenvatinib, cabozantinib, sunitinib, and bevacizumab and ramucirumab.

PARP inhibitors targeting BRCA1/2

It is now well established that some breast (ovarian) cancer patients have a hereditary predisposition to BRCA1/2 deficiency.PARP inhibitors inhibit BRCA1/2-mediated homologous recombinant DNA repair to promote apoptosis of tumor cells, which in turn enhances the efficacy of radiotherapy, as well as alkylating and platinum chemotherapeutic agents. Approved drugs include niraparib, olaparib, Rucaparib and talazoparib.

Targeting CDK4/6 inhibitors

Cyclin-dependent kinases 4/6 (CDK4/6) are a class of serine (Ser)/threonine (Thr) kinases that regulate the cellular transition from G1 to S phase by binding to cytokine D.

Perbociclib (palbociclib) is a CDK4/6 inhibitor that inhibits CDK4/6, thereby blocking tumor cell proliferation.

Drugs targeting mTOR

Phosphatidylinositol 3-kinase/protein kinase B/mammalian target protein of rapamycin (PI3K/Akt/mTOR) is an important signaling pathway existing in the cell, and the PI3K/AKT/mTOR pathway plays an important role in the development of breast cancer. On the one hand, it is downstream of the HER2 pathway, and activation of the PI3K/AKT/mTOR pathway is involved in trastuzumab treatment resistance; on the other hand, it is also interactively activated with the ER signaling pathway, and is involved in the pathogenesis of secondary resistance to endocrine therapy.

Everolimus is an inhibitor of mTOR target protein, and a large number of studies have demonstrated that everolimus reverses aromatase inhibitor resistance by inhibiting PI3K/AKT/mTOR pathway activity. Everolimus combined with trastuzumab in HER2-positive breast cancer is able to reverse trastuzumab resistance and at the same time enhance the antitumor activity of trastuzumab.

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